Objective: The study aims to formulate and evaluate a thermosensitive in Situ gel of erythromycin for the treatment of bullous myringitis. Methods: A thermosensitive in situ gel of erythromycin was optimized for an ideal formulation, which was carried out using the ‘central composite’ design based on prime factors of the formulation, including sol-gel transition temperature, gelling time, in vitro % drug release, and viscosity, using “Design Expert” software and developed by dispersing variable concentrations of Poloxamer 407 and HPMC in distilled water, followed by addition of premixed drug solution in Isopropyl alcohol using constant stirring with a magnetic stirrer. Then, the formulations were stored overnight at 4°C to allow complete hydration of the polymer. All nine formulations were assessed for clarity, sol-gel transition temperature, gelling capacity, drug content, rheological studies, in vitro diffusion study, mucoadhesive strength, pH, ex vivo permeation, and antimicrobial efficacy against Streptococcus pneumoniae and Haemophilus influenzae. Results: All formulations demonstrated satisfactory physicochemical characteristics, including rapid gelling in 21-35 seconds and sol-gel transition temperatures between 32.3 and 42.3ºC. Viscosity tests verified that the substance was appropriate for both delivery and retention, and pH levels between 6.2 and 6.7 were in harmony with the environment of the ear canal. Prolonged residency was supported by mucoadhesive strength, and successful drug transport across the tympanic membrane was demonstrated by ex vivo permeation experiments. Significant inhibition zones against the investigated pathogens were shown by antimicrobial assessment. The best drug content (96.4%), sustained release (92.7±4.8% over 8 hours), high mucoadhesion, and excellent penetration properties were all displayed by ISG9 (19% poloxamer 407 and 1% HPMC). Discussion: The findings of the study suggest that the combination of poloxamer 407 and HPMC effectively produced a thermosensitive in situ gel, which exhibited a rapid sol-gel transition, prolonged retention, sustained drug release, and improved permeation. The optimized formulation (ISG9) also showed good antimicrobial activity, which indicates that it can improve localized treatment and reduce dosing frequency in bullous myringitis. Overall, the results support thermosensitive in situ gel as a promising approach for otic drug delivery. Still, further in vivo and clinical studies are needed to establish its therapeutic potential. Conclusion: The optimized thermosensitive in situ gel (ISG9) showed good gelation, mucoadhesion, sustained release, penetration, and antimicrobial activity, suggesting that it might be used as a novel otic drug delivery method to treat bullous myringitis.
Introduction: Cilnidipine, a calcium channel blocker used to treat hypertension, has poor oral bioavailability owing to extensive first-pass intestinal and hepatic metabolism. Buccal delivery offers an alternative route that bypasses hepatic first-pass metabolism and provides controlled systemic absorption. This study aimed to formulate and optimize a cilnidipine nanoparticle-loaded mucoadhesive buccal tablet using a Quality by Design (QbD) approach. Methods: Cilnidipine polymeric nanoparticles (polyvinylpyrrolidone K-30 with Pluronic F68), prepared by a solvent-evaporation method and characterized in our earlier work, were incorporated into a mucoadhesive matrix of hydroxypropyl methylcellulose (HPMC K4M and HPMC K15M) and Carbopol 934. Tablet hardness and cumulative drug release at 12 h were selected as the critical quality attributes and optimized using an Extreme Vertices Mixture Design (EVMD). Pre- and post-compression parameters, mucoadhesive strength, in vitro dissolution, swelling, release kinetics, and stability under ICH conditions were evaluated. Results: All formulations showed acceptable weight uniformity, hardness, and friability. The optimized formulation (BTF9) achieved 92.2% cumulative drug release over 12 h. The release data best fitted the Higuchi model (R² = 0.994), and the Korsmeyer-Peppas exponent indicated Fickian diffusion. Accelerated stability testing showed no significant change in the key parameters over six months. Discussion: Drug release and mucoadhesion were strongly influenced by polymer composition; the optimized polymer combination prevented burst release and sustained drug release while maintaining adequate mucoadhesion. Conclusion: The nanoparticle-loaded mucoadhesive buccal tablet is a promising candidate for improving the bioavailability of cilnidipine in the management of hypertension. This non-invasive, patient-friendly platform may reduce dosing frequency and improve adherence, and it provides a translational basis for future in vivo and clinical evaluation.
Abstract: Ulcerative Colitis (UC) is a chronic relapsing inflammatory bowel disease characterized by persistent mucosal inflammation of the colon, leading to impaired quality of life and an increased risk of colorectal cancer. Conventional therapies such as amino salicylates, corticosteroids, immunosuppressants, and biologics are effective but are limited by systemic adverse effects, poor site specificity, frequent dosing, and long-term safety concerns. Herbal phytopharmaceuticals have emerged as promising alternatives due to their multi-target anti-inflammatory, antioxidant, immunomodulatory, and mucosal protective actions, with the advantage of standardization and reproducible therapeutic outcomes compared to crude herbal extracts. However, their clinical application is constrained by low solubility, gastrointestinal instability, rapid metabolism, and inadequate localization at inflamed colonic sites. Colon-targeted mucoadhesive microspheres offer a strategic delivery platform by protecting phytopharmaceuticals from gastrointestinal degradation, enhancing mucosal residence time, and enabling localized, sustained drug release in the colon, thereby improving therapeutic efficacy while minimizing systemic exposure. A comprehensive literature search was conducted across PubMed, Scopus, Web of Science, and Google Scholar databases using relevant keywords related to ulcerative colitis, phytopharmaceuticals, colon-targeted drug delivery, and mucoadhesive microspheres. Peer-reviewed articles published primarily in English were critically evaluated to synthesize current evidence and recent advances in this field. This review critically discusses UC pathophysiology, the therapeutic potential of herbal phytopharmaceuticals, and recent advances in colon-specific mucoadhesive microsphere formulations, while addressing formulation challenges, scalability, regulatory considerations, and future prospects, including combination phytopharmaceutical systems, microbiome-responsive delivery, and personalized colon-targeted therapy.
Abstract: Diabetic foot ulcers (DFUs) are considered one of the most debilitating and chronic complications of diabetes mellitus; these ulcers alternate between compromised healing and persistent inflammation, microbial colonization, and biofilm formation. These pathological factors have been known to impair the efficiency of topical treatments and contribute to increased infection and lower limb amputation rates. In recent years, nanotechnology has emerged with innovative nanotechnology-based platforms for topical treatments of chronic wounds; these platforms have focused on nanostructured lipid carriers (NLCs) for topical treatments of chronic ulcers. NLCs consist of a coexistence of solid and liquid lipid particles that have increased stability with the help of surfactants; these particles have proven to be efficient topical drug-delivery systems for chronic ulcers with better capacity for drug entrapment and better skin penetration efficiency. The present review article attempts to make an exhaustive presentation of pathologies of DFUs with special focus on pathologies of bacterial infection and biofilm association and overwhelming pathologies of diabetes-induced chronic inflammation and neuronal impairments. It also attempts to describe NLC with special focus on its penetration efficiency and its association with anti-infection gels for tackling extracellular matrices of biofilm formation at present. It has also attempted to review its safety and biocompatibility with special attention towards biofilm targeting that enhances the penetration efficiency of NLC for deeper penetration of biofilm with sustained drug delivery.
Introduction: Obesity affects hundreds of millions of adults worldwide and represents a major risk factor for metabolic disorders, including type 2 diabetes, cardiovascular disease, and non-alcoholic fatty liver disease. Berberine (BBR) and epigallocatechin gallate (EGCG) are bioactive phytochemicals that exhibit anti-obesity effects through multiple mechanisms, including activation of AMP-activated protein kinase (AMPK), inhibition of lipogenesis, stimulation of thermogenesis, and modulation of the gut microbiota. However, their therapeutic applications are limited by poor oral bioavailability due to low aqueous solubility, chemical instability, and extensive first-pass metabolism, which restrict their absorption and biological efficacy. Methods: A comprehensive literature analysis was conducted on novel nanocarrier platforms, including lipid-based systems (liposomes, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions), polymeric nanoparticles (PLGA, chitosan, protein-based carriers), inorganic nanocarriers, and molecular complexation strategies for BBR and EGCG delivery in obesity models. Results: Recent studies indicate that nano-formulation strategies can substantially enhance the solubility, stability, absorption, and bioavailability of BBR and EGCG compared with conventional formulations. Different nanocarrier systems demonstrate distinct advantages; however, limitations related to formulation stability, scalability, safety assessment, reproducibility, and regulatory approval remain major barriers to clinical application. Preclinical studies suggest that nano-delivered BBR and EGCG may improve metabolic outcomes, including reductions in body weight gain, adiposity, inflammation, and hepatic lipid accumulation, although further validation in well-designed clinical studies is required. Discussion: This review systematically evaluates advanced nano-delivery systems designed to overcome bioavailability barriers of BBR and EGCG, focusing on pharmacokinetic enhancement, targeted delivery, and improved anti-obesity efficacy across preclinical models to inform clinical translation strategies. Conclusion: Nanomedicine-based delivery platforms represent a promising strategy to unlock the anti-obesity therapeutic potential of BBR and EGCG. Future research should focus on the co-delivery of Nanoformulations that utilise the complementary anti-obesity effects of BBR and EGCG and evaluate their clinical feasibility.
