Chronic Obstructive Pulmonary Disease (COPD) remains a major global health burden. Although conventional therapies are effective, they are often associated with systemic side effects, poor target specificity, and cortico...Chronic Obstructive Pulmonary Disease (COPD) remains a major global health burden. Although conventional therapies are effective, they are often associated with systemic side effects, poor target specificity, and corticosteroid resistance. This study emphasizes the therapeutic potential of plant-derived bioactive compounds, when integrated into Nanostructured Drug Delivery Systems (NDDS), for improved COPD management. This is a narrative review based on a comprehensive literature search across major electronic databases (PubMed, Scopus, Web of Science, and Google Scholar) up to July 2025. The analysis focused on phytochemicals with proven anti-inflammatory and antioxidant properties, as well as on nanocarriers such as polymeric nanoparticles, liposomes, and solid lipid nanoparticles, designed to enhance pulmonary targeting and delivery efficiency. Phytochemicals, including curcumin, baicalein, quercetin, berberine, and andrographolide, have shown remarkable efficacy in reducing oxidative stress and inflammation in preclinical COPD models. However, their therapeutic utility is hindered by poor solubility and rapid metabolism. Integration into nanostructured carriers enhanced pulmonary accumulation by 3-6-fold, prolonged drug release up to 24-48 hours, and reduced dosing frequency by approximately 50%, while minimizing systemic toxicity.
Molina-Alejandre O, Villanueva-Martínez NA, Nava-Arzaluz MG
… +10 more, Pérez-Carranza LA, Becerril-Osnaya A, López-Mera GH, Cruz-Morales RD, Sánchez-García D, Martínez-Vieyra I, Chirino YI, Ispanixtlahuatl-Meraz O, Ganem-Rondero A, Cerecedo D
PURPOSE: To compare the antimicrobial effect of Photodynamic (PT) and Sonodynamic Therapy (ST) applying Rose Bengal (RB) loaded in liposomes, intended for the treatment of skin infections. METHODS: Formulations with stan...PURPOSE: To compare the antimicrobial effect of Photodynamic (PT) and Sonodynamic Therapy (ST) applying Rose Bengal (RB) loaded in liposomes, intended for the treatment of skin infections. METHODS: Formulations with standard soy lecithin (TSRB) and water-soluble soy lecithin (TWRB) were prepared and characterized by: (i) FTIR-ATR and DSC, and measuring size, polydispersity index, and zeta potential; (ii) in vitro release and permeation tests, visualizing the distribution of RB in the skin by confocal laser microscopy; (iii) stability tests under different conditions; (iv) occlusion capacity tests; (v) determination of antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa; and (vi) cytotoxicity tests with HaCaT keratinocytes. RESULTS: Both formulations exhibited encapsulation rates > 93% and particle sizes < 100 nm. TWRB was more stable, delaying RB release (12.8 % at 8h) and facilitating its penetration into the skin. MRSA was inhibited with PT and ST. P. aeruginosa was inhibited with TWRB/ST. Viability was >80% in HaCaT keratinocytes treated with TWRB/PT; however, acoustic cavitation caused significant cell detachment, precluding cytotoxicity assessment in ST assays. DISCUSSION: TWRB exhibited good technological and stability properties, capable of delaying RB release while enhancing its penetration into the skin. Although MRSA (Gram-positive) was inhibited, the most interesting results were obtained with P. aeruginosa (a Gram-negative bacterium, difficult to eradicate), as TWRB/ST completely inhibited it at a lower concentration than the RB solution. CONCLUSION: The results, particularly with P. aeruginosa, provide a basis for further studies using this system.
INTRODUCTION: The fourth major cause of death worldwide is Neurodegenerative Diseases (NDs), including Alzheimer's and Parkinson's disease. The existing therapies have only a small effect on alleviating symptoms, mainly...INTRODUCTION: The fourth major cause of death worldwide is Neurodegenerative Diseases (NDs), including Alzheimer's and Parkinson's disease. The existing therapies have only a small effect on alleviating symptoms, mainly because the therapeutic agents are difficult to cross the bloodbrain barrier. The purpose of the review is to discuss the potential of microneedle-based transdermal delivery systems to improve the delivery of drugs to the central nervous system and thereby manage neurodegenerative diseases effectively. METHODS: The article summarizes and synthesizes the available literature that targets the strategies of microneedle-mediated drug delivery. The literature on the design, composition, pharmacokinetics, and mechanistic benefits of different microneedle platforms for surmounting central nervous system barriers was identified and thematically synthesized. RESULTS: Microneedle systems have emerged as non-invasive delivery systems with the potential for localized and sustained drug delivery, overcoming the stratum corneum and the blood-brain barrier. Micro-needles can be used to deliver small molecules, peptides, and nanoparticles to the brain, thereby avoiding systemic side effects and enhancing drug bioavailability. Some of those designs include dissolving, coated, hollow, hydrogel-forming, and stimuli-responsive microneedles, which have been shown to target the brain and exhibit higher therapeutic efficiency in preclinical models. DISCUSSION: Although technological advances have improved, the clinical translation of microneedlebased strategies remains limited. The future directions could include using microneedles with stem cell-based therapies, CRISPR/Cas9 gene editing, artificial intelligence-based delivery systems, and responsive release technology to facilitate customized treatment. CONCLUSION: The Microneedle-based drug delivery systems are promising in overcoming the current limitations in the treatment of neurodegenerative diseases. Nonetheless, a large-scale clinical validation is necessary to guarantee safety, efficacy, and scalability to be applied to real-life scenarios.
INTRODUCTION: Pyridine-based derivatives are well-known for their broad-spectrum therapeutic applications, particularly as antimicrobial and antioxidant agents. However, clinical utility is often hindered by poor aqueous...INTRODUCTION: Pyridine-based derivatives are well-known for their broad-spectrum therapeutic applications, particularly as antimicrobial and antioxidant agents. However, clinical utility is often hindered by poor aqueous solubility and limited bioavailability. This study aimed to synthesize and evaluate the biological activity, pharmacokinetic properties, and nanoparticle-based enhancement of a novel furo[2,3-b]pyridine derivative. METHODS: Ethyl 3-amino-4-(4-methoxyphenyl)-6-(p-tolyl)furo[2,3-b]pyridine-2-carboxylate (compound 3) was synthesized and structurally characterized using NMR, FT-IR, MS, and UV-Vis spectroscopy. Molecular docking studies were conducted to assess binding interactions with methionyltRNA synthetase (PDB ID: 3KFL) and xanthine oxidoreductase (PDB ID: 1R4U). ADME parameters were predicted using SwissADME. To improve solubility, silver nanoparticles (AgNPs) were synthesized using Compound 3 and characterized via scanning electron microscopy (SEM). In vitro antimicrobial and antioxidant assays were performed to validate in silico findings. RESULTS: Docking simulations revealed strong binding affinities of compound 3 to both target enzymes, supporting its potential antimicrobial and antioxidant roles. ADME analysis demonstrated a favorable pharmacokinetic profile, with high gastrointestinal absorption, acceptable bioavailability, and compliance with Lipinski and related drug-likeness rules, but consistently poor solubility predictions across multiple models. The synthesized AgNPs exhibited a size range of 44-64 nm and significantly enhanced the solubility and stability of compound 3. In vitro assays demonstrated that the AgNPs exhibited superior antimicrobial activity, particularly against Staphylococcus aureus and Bacillus subtilis, and a marked increase in antioxidant potential, achieving 64.62% radical scavenging activity compared to 16.49% for the free compound. DISCUSSION: The integration of nanotechnology with pyridine-based pharmacophores effectively addressed the limitations of solubility and bioavailability. The enhanced biological efficacy of AgNPs underscores their potential as multifunctional therapeutic agents targeting microbial infections and oxidative stress. CONCLUSION: This study presents a promising nanoparticle-assisted strategy to enhance the therapeutic potential of pyridine-based compounds. The dual antimicrobial and antioxidant activities of furo[2,3- b]pyridine-based AgNPs offer a valuable platform for the deve.
Extracellular vesicles (EVs), encompassing exosomes, microvesicles, and apoptotic bodies, are pivotal mediators of intercellular communication, facilitating the transfer of nucleic acids, proteins, and lipids between cel...Extracellular vesicles (EVs), encompassing exosomes, microvesicles, and apoptotic bodies, are pivotal mediators of intercellular communication, facilitating the transfer of nucleic acids, proteins, and lipids between cells and thereby influencing a wide range of physiological and pathological processes. Their inherent biocompatibility, nanoscale size, and ability to reflect the molecular signatures of their parental cells have positioned EVs as promising therapeutic agents for various diseases, including neurological, cardiovascular, hepatic, and pulmonary disorders, for which conventional therapies often provide limited or nonspecific benefits. Notably, EVs can traverse biological barriers such as the blood-brain barrier, enhancing their clinical applicability by enabling drug delivery to anatomically protected sites. Furthermore, patient-derived EVs exhibit distinct molecular profiles compared with healthy controls, underscoring their potential as diagnostic biomarkers and modulators of disease pathogenesis, with growing evidence demonstrating their ability to distinguish disease subtypes, predict prognosis, and monitor therapeutic responses. Accumulating evidence also indicates that EVs regulate immune responses, angiogenesis, and tissue remodeling, thereby contributing to both physiological homeostasis and pathological processes. Engineered EVs further offer innovative drug delivery solutions by improving therapeutic precision while minimizing adverse effects associated with conventional systems, and they hold considerable promise for future personalized- medicine strategies. This review summarizes current knowledge on the diverse roles of EVs across major organ diseases, highlights their translational potential as both therapeutic agents and biomarkers, and discusses emerging challenges that must be addressed for successful clinical translation. By providing a comprehensive overview, this study aims to advance the clinical translation of EVs in precision medicine.
INTRODUCTION: Brain cancer treatment is hindered by the complexity of the brain and the restrictive nature of the blood-brain barrier (BBB), which limits the efficacy of anticancer drugs. This study aimed to enhance the...INTRODUCTION: Brain cancer treatment is hindered by the complexity of the brain and the restrictive nature of the blood-brain barrier (BBB), which limits the efficacy of anticancer drugs. This study aimed to enhance the delivery of Docetaxel (DTX) for brain cancer treatment through intranasal administration using mucoadhesive polymer coatings on poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs). Intranasal delivery bypasses the BBB, providing a direct nose-to-brain route with faster drug action. Enhancing mucoadhesion and drug permeation could improve drug bioavailability and therapeutic outcomes while reducing systemic side effects. METHODS: DTX-loaded PLGA NPs were prepared and coated with chitosan (CS), carboxymethyl chitosan (CMCS), and glycol chitosan (GCS). The NPs were characterized for particle size, surface charge, morphology, encapsulation efficiency (EE%), and loading capacity (LC%). Mucoadhesion and drug release profiles were evaluated in vitro, while pharmacokinetic studies were performed in vivo using rats. RESULTS: The coated NPs had sizes ranging from 209.33 to 339.94 nm with a positive surface charge, spherical shape, and smooth surfaces. Encapsulation efficiency exceeded 98.88%, and loading capacity ranged from 45.23% to 48.83%. In vitro studies confirmed enhanced mucoadhesion and biphasic drug release patterns. Pharmacokinetic analysis in rats showed significantly improved drug absorption, with higher Cmax and AUC0-∞ values for coated NPs compared to uncoated NPs and nonformulated DTX. DISCUSSION: DTX absorption through the nasal mucosa is enhanced, possibly due to the mucoadhesive and permeation-enhancing characteristics of CS and its derivatives. While promising, further studies including efficacy and safety evaluations are needed. CONCLUSION: DTX-loaded PLGA NPs coated with CS, CMCS, and GCS demonstrated enhanced mucoadhesion, improved pharmacokinetics, and superior nasal mucosal absorption. This approach holds potential for targeted brain cancer therapy by reducing dosage requirements and minimizing systemic side effects.
INTRODUCTION: Exosomes, nanosized extracellular vesicles secreted by diverse cell types, have emerged as promising natural nanocarriers for therapeutic delivery. Their intrinsic ability to cross the Blood-Brain Barrier (...INTRODUCTION: Exosomes, nanosized extracellular vesicles secreted by diverse cell types, have emerged as promising natural nanocarriers for therapeutic delivery. Their intrinsic ability to cross the Blood-Brain Barrier (BBB) positions them as valuable tools for treating neurodegenerative diseases. This review critically examines exosome biology, transport mechanisms, engineering strategies, and their clinical potential as drug-delivery platforms for the Central Nervous System (CNS). METHODS: We analyzed recent experimental, translational, and clinical studies on exosomes and engineered derivatives, focusing on BBB penetration, therapeutic cargo delivery, and applications in brain disorders. Key advances and landmark preclinical studies were synthesized to provide a comprehensive perspective. RESULTS: Exosomes cross the BBB through receptor-mediated transcytosis, lipid raft-associated uptake, and macropinocytosis, enabling bidirectional transport between circulation and brain. Their intrinsic cargo, including proteins, nucleic acids, and lipids, can reflect disease states and serve as predictive biomarkers. Engineered exosomes further enhance delivery potential, as surface functionalization and optimized cargo loading improve brain specificity and therapeutic efficacy in preclinical models. Collectively, both native and engineered exosomes surpass many synthetic carriers in stability, targeting, and BBB penetration. DISCUSSION: Versus previous reviews, this manuscript integrates exosome composition, engineering, isolation technologies, and administration routes, while also addressing patent and clinical translation challenges. Importantly, it highlights quantitative and mechanistic insights into BBB transport, offering a distinct framework for advancing exosome-based CNS therapies. CONCLUSION: Exosomes constitute a versatile platform for BBB-crossing drug delivery. By consolidating mechanistic, preclinical, and translational evidence, this review highlights their transformative potential in neurodegenerative disease therapy while outlining limitations and future directions.
INTRODUCTION: Ulcerative colitis requires targeted therapy to enhance efficacy and minimize systemic side effects. This study aimed to address the low bioavailability and nonspecific release of naringin, a natural anti-i...INTRODUCTION: Ulcerative colitis requires targeted therapy to enhance efficacy and minimize systemic side effects. This study aimed to address the low bioavailability and nonspecific release of naringin, a natural anti-inflammatory flavonoid, by developing a colon-targeted delivery system for ulcerative colitis treatment. METHODS: The pill core was prepared via a melt-dropping method and optimized using orthogonal experimental design. The pH/enzyme dual-responsive coating was refined using Box-Behnken response surface methodology. In vitro release was evaluated in a gradient pH model (gastric pH 1.2, intestinal pH 6.8, colonic pH 7.6) with enzymatic tolerance tests. RESULTS: The optimal core conditions were a drug-to-matrix ratio of 1:3, melting temperature of 90°C, and condensation temperature of 5°C, producing pills with 33% drug loading and excellent sphericity. The optimized coating contained 1.6% dibutyl phthalate and 0.80% ethyl cellulose, and achieved 20.60% weight gain. The formulation exhibited <20% cumulative release in gastric and intestinal fluids, and approximately 75-78% release in colonic fluid within 10 hours. Release kinetics best fit the Weibull model (R² = 0.9785), indicating a diffusion-controlled mechanism. DISCUSSION: This dual-responsive system overcomes the limitations of single-trigger colon-targeted formulations due to individual variability, ensuring colon-specific delivery. However, the static dissolution model may not fully replicate the dynamic colonic environment, and in vivo studies are needed to confirm therapeutic efficacy. CONCLUSION: A pH/enzyme dual-responsive dropping pill system for colon-targeted naringin delivery was successfully developed and optimized. The formulation showed promising in vitro release profiles and holds potential for localized treatment of ulcerative colitis.
INTRODUCTION: Muscle relaxants are fundamental to modern anesthesia, primarily targeting voltage-gated sodium channels. While μ-conotoxin CnIIIC is a potent peptide inhibitor, its clinical translation is hindered by poor...INTRODUCTION: Muscle relaxants are fundamental to modern anesthesia, primarily targeting voltage-gated sodium channels. While μ-conotoxin CnIIIC is a potent peptide inhibitor, its clinical translation is hindered by poor metabolic stability and rapid systemic clearance. This study aimed to overcome these limitations and enhance its therapeutic potential via a rational molecular self-assembly strategy. METHODS: Two novel derivatives of μ-conotoxin CnIIIC (S1-CnIIIC and S2-CnIIIC) were designed and synthesized through site-specific side-chain modification. Their self-assembly properties were systematically characterized, and their efficacy was evaluated in a mouse model by measuring the duration of neuromuscular blockade, which was compared against the native peptide. RESULTS: S1-CnIIIC demonstrated a moderate propensity for self-assembly. In contrast, S2-CnIIIC efficiently formed micellar structures with a critical micelle concentration of 524.8 μM, indicating a superior self-assembly capability. In vivo, S2-CnIIIC not only exhibited a significantly prolonged duration of neuromuscular blockade but also showed a reduced systemic toxicity profile compared to the native CnIIIC. DISCUSSION: The molecular self-assembly approach markedly enhanced the stability and overall pharmacological performance of the peptide inhibitor. Our findings indicate that side-chain engineering effectively modulates the supramolecular assembly process, which in turn facilitates a more controlled drug release kinetics. The exceptional in vivo performance of S2-CnIIIC underscores the potential of rationally designed peptide nanostructures to address key challenges in peptide-based drug development. CONCLUSION: Molecular self-assembly presents a robust strategy to advance the clinical translation of μ-conotoxin derivatives. Specifically, the S2-CnIIIC derivative emerges as a highly promising candidate for next-generation muscle relaxants, successfully combining a prolonged neuromuscular blockade with an improved safety profile.
INTRODUCTION: Ulcerative colitis (UC) is a chronic inflammatory bowel disease with an increasing global incidence. Current clinical therapies are often limited by insufficient efficacy and adverse effects, highlighting t...INTRODUCTION: Ulcerative colitis (UC) is a chronic inflammatory bowel disease with an increasing global incidence. Current clinical therapies are often limited by insufficient efficacy and adverse effects, highlighting the urgent need for safe and effective treatment strategies. This study aimed to develop a colon-targeted drug delivery system based on a "nano-in-micro" strategy for UC therapy. METHODS: Baicalein nanocrystal microspheres (BE-NC MS) were prepared using an emulsification- internal gelation method. Their morphology, particle size, Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (XRD) were characterized. In vitro drug release behavior was evaluated. A dextran sodium sulfate (DSS)-induced UC model was established in C57BL/6 mice, and therapeutic efficacy was assessed after 7 days of treatment. RESULTS: BE MS and BE-NC MS exhibited uniform particle sizes of 186.22 ± 0.69 μm and 185.49 ± 0.38 μm, respectively. The drug was effectively encapsulated and successfully delivered to the colon. Compared with baicalein (BE), baicalein nanocrystals (BE-NC), and (Baicalein microspheres) BE MS, BE-NC MS significantly alleviated UC symptoms and markedly reduced the levels of TNF-α, IL-1β, and IL-6 in colon tissue. DISCUSSION: The enhanced therapeutic efficacy of BE-NC MS may be attributed to colon-specific delivery and improved bioavailability provided by the nano-in-micro formulation, enabling effective suppression of colonic inflammation. CONCLUSION: BE-NC MS represents a promising colon-targeted delivery system and offers a potential new strategy for the treatment of ulcerative colitis.
BACKGROUND: The majority of post-procedure skin whitening and repair methods for postmedical aesthetic procedures fail to achieve desired skin whitening and repair functionality due to limitations in stability and skin p...BACKGROUND: The majority of post-procedure skin whitening and repair methods for postmedical aesthetic procedures fail to achieve desired skin whitening and repair functionality due to limitations in stability and skin penetration capability. OBJECTIVE: To address this issue, we developed a Triple Permeation System (TPS) integrated nanocarrier, atomization, and electro-enhanced permeation technologies. METHODS: Five active ingredients were encapsulated into the liposomes via high-pressure homogenization technology to form a composite nanocarrier named PRO-Peptide311. RESULTS: PRO-Peptide311 effectively increased cellular uptake and significantly decreased tyrosinase activity, melanin expression, ROS levels, and the secretion of inflammatory factors at the cellular level. Moreover, the skin whitening efficacy was confirmed using a 3D skin model. When combined with atomization and electro-enhanced permeation technologies, PRO-Peptide311 demonstrated substantially improved percutaneous penetration compared to any single technology alone. DISCUSSION: The enhanced performance of TPS highlights the synergistic effect achieved through combining nanocarrier encapsulation with physical enhancement techniques. This integrated approach effectively overcomes key limitations in transdermal delivery, such as poor stability and insufficient penetration of multi-functional active compounds. The system shows strong potential for application in managing post-inflammatory hyperpigmentation and lays the foundation for the future development of advanced skincare delivery systems. CONCLUSION: The TPS-based delivery system not only alleviates post-inflammatory hyperpigmentation following aesthetic procedures but also holds promise for broadening the scope of transdermal therapies in dermatology and cosmeceuticals.
INTRODUCTION: studies have demonstrated the wound-healing effects of tazetta L. bulb. This study investigates the wound healing effect of different topical niosomal creams and gel of the standardized extract of bulb i...INTRODUCTION: studies have demonstrated the wound-healing effects of tazetta L. bulb. This study investigates the wound healing effect of different topical niosomal creams and gel of the standardized extract of bulb in an animal model. METHODS: Niosomes were prepared by the thin film hydration method using percolated extraction of bulbs and characterized pharmaceutically. Two niosomal (Span/Tween 40 with alcoholic plant extract and Span/Tween 60 with aqueous botanical extract lipid vesicles) creams and gels containing aqueous or alcoholic bulb extract were investigated in wound healing in male Wistar rats compared to Alpha® ointment. RESULTS: The mean volume diameter of prepared niosomes was between 6.87 and 18.70 μm, 48 hours after preparation. The niosomal formulations of bulb extract, whether in cream or gel form, enhance wound healing by enabling advanced penetration of encapsulated herbal compounds. DISCUSSION: On the 7th day after wound formation, the wound surface of the cream and gel groups had a significant decrease compared to the control group, but on the 9 day, a significant difference was observed only between the gel group and the control group. On the 11 day, the wound surface area reduction of Alpha® ointment, free extract, and niosomal gel groups was significantly different from the control group. CONCLUSION: Niosomal formulations of bulb has potential for pharmaceutical and cosmeceutical applications, which require further animal and clinical studies to determine the mechanism of action and potential side effects.
INTRODUCTION: Retinitis Pigmentosa (RP), an inherited retinal disease, characterized by a progressive loss of photoreceptor cells, leading to vision impairment. Mutations in the pre-mRNA processing factor gene (PRPF31) m...INTRODUCTION: Retinitis Pigmentosa (RP), an inherited retinal disease, characterized by a progressive loss of photoreceptor cells, leading to vision impairment. Mutations in the pre-mRNA processing factor gene (PRPF31) major cause of autosomal dominant RP. While viral vectors like AAV are commonly used in gene therapy, they are limited by low DNA cargo capacity and immunogenicity. We aimed to develop a chitosan-based NPs to deliver PRPF31 plasmid DNA (pDNA) into the ARPE-19 retinal cell line. METHODS: The Complex coacervation method was used to prepare CS NPs loaded with PRPF31. The NPs were characterized for particle size, polydispersity index (PDI), and zeta potential using a zetasizer. Surface morphology of CS-based NPs was examined using SEM. Additionally, the loading capacity, encapsulation efficiency, protective effect of CS on the pDNA, in vitro transfection efficiency, and cytotoxicity were evaluated in ARPE-19 cell lines Results: The particle size, PDI, and zeta potential of chitosan nanoparticles were 245.19 ± 21.27nm, 0.265 ± 0.023, and +20.5 ± 5.63 mV, respectively. Scanning Electron Microscopy (SEM) images confirmed the formation of NPs. The pDNA encapsulation efficiency was 66.80%± 4.69 and a loading efficiency of 21.93%± 1.08. The transfection efficiency of naked pDNA in ARPE-19 cells was 24.40% while that of CS pDNA NP was 48.30%. Cells transfected with pDNA using the standard transfecting agent Lipofectamine showed a higher transfection efficiency of 65.24% as compared to both naked pDNA and CS-pDNA NPs. DISCUSSION: Cs- pDNA particles demonstrated moderate transfection efficiency and lower cytotoxicity in the retinal cell line. In vivo research is required to realize its future therapeutic potential. CONCLUSION: These CS-pDNA NPs may have potential as a non-viral delivery vehicle in gene therapy in RP, however, further research in animal models is needed to validate the in vitro findings and for their potential therapeutic applications.
The solubility of pharmaceutical compounds is a pivotal determinant of their bioavailability and therapeutic effectiveness. Many promising drugs face significant solubility challenges, hindering their clinical applicatio...The solubility of pharmaceutical compounds is a pivotal determinant of their bioavailability and therapeutic effectiveness. Many promising drugs face significant solubility challenges, hindering their clinical application. This review focuses on innovative solid dispersion techniques to enhance drug solubility. Solid dispersions involve the distribution of active pharmaceutical ingredients within a polymeric matrix, which can markedly improve dissolution rates and overall solubility. Various preparation methods, including melt extrusion, solvent evaporation, and spray drying, are critically examined for their effectiveness across different drug formulations. The role of carriers, namely hydrophilic polymers and surfactants, is emphasized in facilitating solubilization and enhancing drug stability. Furthermore, we discuss the implications of these techniques on the pharmacokinetic profiles of selected drugs, supported by recent advancements in characterization methods that aid in understanding the physicochemical properties of solid dispersions. This review underscores the significance of solid dispersion techniques in pharmaceutical formulation, paving the way for the development of more effective therapeutic agents. Future research directions are proposed, highlighting the need for optimization of these techniques and exploration of novel materials to further improve drug solubility and bioavailability.
INTRODUCTION: Acne vulgaris is a prevalent dermatological disorder that affects millions worldwide, causing both physical discomfort and psychological burden. Conventional therapies often provide limited benefit due to p...INTRODUCTION: Acne vulgaris is a prevalent dermatological disorder that affects millions worldwide, causing both physical discomfort and psychological burden. Conventional therapies often provide limited benefit due to poor skin permeability and tolerability issues. METHODS: This study covers indepth literature study (2000-2025) on Adapalene in acne treatment. Closely related 150 studies on innovative nanocarriers and the role of AI in Drug Delivery were included, while unrelated works were excluded. RESULTS: Although adapalene demonstrates strong anti-acne activity, its limited membrane permeability and local dermatological adverse reactions restrict clinical effectiveness. Nanocarrier-based systems resolved these issues by enhancing drug penetration and controlled release, as evidenced by case studies and major clinical trials. ANN-assisted optimization further refined drug delivery, enabling more effective and personalized management of acne. DISCUSSION: Adapalene is a promising therapeutic agent for acne vulgaris; however, its limited pharmacokinetic profile restricts its effectiveness. The integration of nanotechnology and AI-driven optimization could significantly improve its therapeutic potential, a concept further supported by findings from various clinical studies. CONCLUSION: Adapalene-loaded nanocarriers represent a promising approach for improving therapeutic outcomes in acne treatment. Integration of AI-based optimization with clinical validation highlights its translational potential, paving the way toward safer, more efficient, and patient-specific dermatological therapies.
Curr Drug Deliv
· 2026 Mar · PMID 41926309
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After several decades of research and development, liposomes have found many interesting applications in different disciplines of science, from biology to colloid science, tissue engineering, and regenerative medicine, a...After several decades of research and development, liposomes have found many interesting applications in different disciplines of science, from biology to colloid science, tissue engineering, and regenerative medicine, and, more importantly, drug delivery, i.e., one of the most exciting fields of application and innovation where Ehrlich's concept of a "magic bullet" has remained viable. This focus on liposomal drug delivery systems can be attributed in part to the phospholipid bilayer structure of these vesicles, which resembles the architecture of the eukaryotic cell membrane. Many liposomal drug carriers are being developed, and some of them, such as DOXIL, have also been commercialized. Drug-loaded liposomes can be prepared and the desired characteristics of the final formulation. However, these products face two significant challenges: the presence of free, nonencapsulated drug molecules, which must often be removed, and limited drug-loading efficiency. Currently, no universal method exists to address either issue fully. This review aims to provide a comprehensive overview of strategies to enhance drug entrapment and remove free, non-encapsulated drug from liposomal formulations, to compare the advantages and limitations of current methods, and to identify remaining knowledge gaps to guide future research and formulation design. To this end, the first section describes drug loading methods, followed by purification techniques, with an emphasis on recently developed approaches and their specific benefits and drawbacks.
Momeni J, Hosseini E, Sahraian MA
… +1 more, Negah SS
Curr Drug Deliv
· 2026 Mar · PMID 41918199
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One of the main bottlenecks in regenerative therapy is low neuronal differentiation after stem cell transplantation. Several approaches can induce neuronal differentiation, such as transcription factor manipulation, grow...One of the main bottlenecks in regenerative therapy is low neuronal differentiation after stem cell transplantation. Several approaches can induce neuronal differentiation, such as transcription factor manipulation, growth factors and cytokines, optogenetics, metabolic reprogramming, and Small Molecules (SMs). Each method has advantages and disadvantages; however, shortening the induction time and the maximum rate of neuronal differentiation is a high priority when selecting a method. Among all approaches, SMs can match these properties. Furthermore, SMs can target the developmental signaling pathways in neuronal maturation and generation. For example, they modulate WNT, Notch, TGF-β/SMAD, Sonic Hedgehog (Shh), FGF, Retinoic Acid, MAPK/ERK, PI3K/AKT/mTOR, cAMP/PKA, BMP, JAK/STAT, and Nrf2 pathways. These pathways are essential for regulating neuronal differentiation, and SMs serve as a powerful tool for manipulating them in both research and therapeutic contexts. Therefore, we examine recent studies on SMs and discuss the pitfalls and challenges encountered during neuronal differentiation in preclinical research. Additionally, we review relevant studies that have advanced to clinical stages. Ultimately, based on our findings, we conclude that SMs hold significant promise for inducing neurons from stem cells; however, comprehensive clinical studies are necessary to demonstrate their efficacy in stem cell therapy for neurological disorders.
Sahoo BM, Sharma S, Bhatnagar P
… +2 more, Saraogi GK, Banik BK
Curr Drug Deliv
· 2026 Mar · PMID 41918198
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Glycosylation plays a significant part in cancer pathophysiology, shaping tumour progression, metastasis, immune evasion, and drug resistance. Aberrant glycosylation patterns in tumours serve as impending biomarkers and...Glycosylation plays a significant part in cancer pathophysiology, shaping tumour progression, metastasis, immune evasion, and drug resistance. Aberrant glycosylation patterns in tumours serve as impending biomarkers and therapeutic targets for enriched cancer diagnostics and treatment strategies. Developments in glycosylation-mediated drug delivery systems (DDSs) have enabled more targeted targeting of tumour cells through receptor-specific interactions, boosting drug efficacy while mitigating systemic toxicity. Glycosylated nanocarriers, antibodies, and fusion proteins have proven favourable applications in anticancer therapies, improving drug stability, cellular uptake, and immune modulation. Recent patents focus on innovative advances leveraging glycosylation to improve drug targeting, stability, and therapeutic efficacy, predominantly in addressing multidrug resistance in cancers such as non-small cell lung cancer, breast cancer, and prostate cancer. Narrative review, synthesizing published research and patents related to glycosylation-mediated drug delivery for cancer. Peer-reviewed journal articles and patents retrieved from European, Google Patents, and Lens.org databases (2020-2025) using keywords such as . Covers glycosylation biology in cancer, receptor-mediated targeting, applications in nanocarriers and antibodies, roles in metastasis, immune evasion, metabolism, ferroptosis, senescence, biomarkers, and delivery systems. Qualitative synthesis of literature findings and patent specifications, categorizing them by therapeutic approach, target, stage of development, and potential for clinical translation. Identification of trends, challenges, and future perspectives in glycosylation-based drug delivery. This review surveys the structural and functional aspects of glycosylation in cancer biology, its effects on tumour behaviour, and its emerging role in personalised medicine through glycosylation-based diagnostics and targeted therapeutics.
In the published version of this article, a discrepancy was identified in the reference numbers provided in Table 7. Citations within Table 7 were numbered up to [228], whereas the article's reference section contained o...In the published version of this article, a discrepancy was identified in the reference numbers provided in Table 7. Citations within Table 7 were numbered up to [228], whereas the article's reference section contained only 224 entries. This inconsistency occurred due to an error in reference numbering during the final preparation of the manuscript. The numbering in Table 7 has now been corrected to align accurately with the reference list. This correction does not affect the article's scientific content, data interpretation, or conclusion. The original article can be found online at: https://www.benthamscience.com/article/145714 The publisher apologizes for this oversight and any inconvenience caused to the authors and readers.
Islam I, Ullah K, Khan SA
… +3 more, Yasin H, Ali S, Murtaza G
Curr Drug Deliv
· 2026 Feb · PMID 41691695
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INTRODUCTION: Conventional treatment of colorectal cancer causes severe side effects, leading to non-compliance. Hydrogels are polymer-based oral drug delivery carriers that offer numerous advantages. METHODS: This study...INTRODUCTION: Conventional treatment of colorectal cancer causes severe side effects, leading to non-compliance. Hydrogels are polymer-based oral drug delivery carriers that offer numerous advantages. METHODS: This study describes the application of the free-radical polymerization approach for the synthesis of colon-targeted, pH-responsive, pullulan-co-MAA hydrogels to deliver 5-fluorouracil. The prepared hydrogels were characterized in vitro and in vivo. RESULTS: In vitro characterizations confirmed successful crosslinking, a decrease in the drug's crystallinity, a rough morphology, and the stable nature of the drug. Gel content, swelling index, porosity, and drug entrapment efficiency were increased with the increase in the concentration of polymer and monomer. The drug release followed a swelling study pattern; the cumulative drug release was increased with the increase in concentration of polymer (80.4% to 95.6%) and monomer (72.1% to 78.3%), while cross-linker negatively affected the drug release (62.2% to 53.5%) at pH 7.4. The results of the MTT-assay showed that blank hydrogels were cyto-compatible as all the cells displayed more than 95% viability, while drug-loaded hydrogels exhibited dose dose-dependent cytotoxic effect. Oral tolerability results showed that the hydrogel suspension was well-tolerated up to 4000mg/kg of body weight without altering hematology and serum chemistry profile or tissue histology of various organs. DISCUSSION: The results confirmed successful hydrogel formation with effective 5-fluorouracil entrapment, enhanced thermal stability, and controlled drug release influenced by the concentrations of polymer, monomer, and crosslinker. CONCLUSION: According to findings, the fabricated hydrogels have promising potential to deliver 5- fluorouracil and other hydrophilic moieties into the colon.