Journal of Pharmaceutical Innovation最新文献

{"title":"Repurposing Esmolol for Diabetic Wound Healing: Formulation Development, In-Silico and In-Vivo Evaluation in Diabetic Rats","authors":"Rahul Padalkar,&nbsp;Ashwini Madgulkar,&nbsp;Sudhir Kulkarni,&nbsp;Rutuja Sultanpure,&nbsp;Shrawani Nighot,&nbsp;Shreyas Barde","doi":"10.1007/s12247-025-10085-6","DOIUrl":"10.1007/s12247-025-10085-6","url":null,"abstract":"<div><p>Diabetic wounds are challenging to heal due to multiple pathologies in the wound healing process. The complex cellular environment surrounding diabetic wounds impairs the functioning of vital cells, including vascular endothelial cells, fibroblasts, and epithelial cells, which are essential for wound healing, thereby hindering the repair process. The present work demonstrates the potential of esmolol hydrochloride in diabetic wound healing through molecular docking studies and hydrogel formulation along with D-panthenol. Esmolol hydrochloride exhibited significant binding affinity withCaspase-8, MMP1 and MMP8. Esmolol hydrochloride did not show any cytotoxic effect in the MTT assay at concentrations up to 250uM. Based upon these observations, esmolol(14%) was formulated into a hydrogel (WHG) along with D-panthenol (5%). The formulation was evaluated for wound healing activity in streptozotocin-induced diabetic rats through the excision wound model. The WHG group showed almost 96% wound closure at the end of 21 days. At various times during this study period, wound tissues were examined for histopathological changes. Cell proliferation, remodeling and collagen building observed in the WHG group suggested excellent progress of wound healing. A considerable increase in hydroxyproline and hexosamine levels was also observed during the study period, indicating collagen and extracellular matrix synthesis. The combination index value of 1.02 indicated additive effect of both the actives in wound healing. These findings suggest that esmolol and D-panthenol hydrogel can serve as a promising approach for diabetic wound healing.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145256833","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design and Development of Butyrosomes as Novel Carriers Using Lipid Isolated from Diploknema butyracea (Roxb.) H. J. Lam","authors":"Abhishek Anand,&nbsp;Jyoti Saini,&nbsp;Nitish Singh Jangwan,&nbsp;Gaurav Kumar Jain,&nbsp;Anoop Kumar,&nbsp;Surajpal Verma,&nbsp;Devesh Tewari","doi":"10.1007/s12247-025-10099-0","DOIUrl":"10.1007/s12247-025-10099-0","url":null,"abstract":"<div><h3>Purpose</h3><p>Lipids are widely used as nanocarriers for drug delivery, but selecting an appropriate lipid remains a major challenge. Natural lipids provide a safer, more sustainable alternative over synthetic lipids. <i>Diploknema butyracea</i> (Roxb.) H. J. Lam a sub-Himalayan tree of India and Nepal yields Cheura lipid. This is the first study that investigates the use of Cheura lipid for the development of SLNs (butyrosomes) using sertaconazole nitrate (STZN) as model drug, along with a comprehensive technical characterization.</p><h3>Methods</h3><p>A QbD based Box–Behnken Design was employed to develop butyrosomes using Cheura lipid, for particle size and PDI. TEM was used to examine the morphology and distribution of the nanoparticles. The %EE, and in-vitro drug release profiles were evaluated to determine the STZN-butyrosomes release behaviour. Comprehensive physiochemical, spectroscopical, microscopical, diffractometry, rheological and thermogravimetric characterization was performed.</p><h3>Results</h3><p>The optimized STZN-butyrosomes showed a particle size (230 nm), PDI (&lt; 0.5), a zeta potential (– 25.7 ± 0.6 mV), and a % EE (97.04%). TEM confirmed a spherical morphology with uniform distribution. The in-vitro drug releases reached 98.49% over 24 h. The raw lipid showed high saturation, an amorphous structure, characteristic functional groups, and uniform droplets (300–400 nm). Elemental analysis confirmed the absence of toxic heavy metals and the presence of essential trace elements. Thermal stability was maintained up to 300 ℃.</p><h3>Conclusion</h3><p>The study suggests that Cheura lipid is a natural, safe, with potential as a nanocarrier for delivery systems such as SLNs, NLCs, niosomes, phytosomes, and nanoemulsions, making it a promising material in nanotechnology.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145256273","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Repurposing Sulfonamide-Based Antidiabetic Agents Against Polycystic Ovary Syndrome: A Molecular Docking and Dynamics Simulation Approach","authors":"Miah Roney,&nbsp;Abdul Rashid Issahaku,&nbsp;S. M. Istiaque Hamim,&nbsp;Anke Wilhelm,&nbsp;Mohd Fadhlizil Fasihi Mohd Aluwi","doi":"10.1007/s12247-025-10119-z","DOIUrl":"10.1007/s12247-025-10119-z","url":null,"abstract":"<div><p>Polycystic ovary syndrome (PCOS) is a prevalent endocrine disorder affecting women of reproductive age, marked by hyperinsulinemia, hyperandrogenism, menstrual irregularities, and long-term metabolic complications. Cytochrome P450 17A1 (CYP17A1) is a key enzyme in the biosynthesis of adrenal and gonadal steroids, and its overexpression leads to enhanced conversion of androgens into testosterone, contributing to hyperandrogenism. Targeting CYP17A1 activity presents a viable strategy to mitigate androgen production in the ovaries. In this study, sulfonamide-based antidiabetic drugs were evaluated through molecular docking to identify potential CYP17A1 inhibitors. Among the candidates, Chlorpropamide and Tolazamide demonstrated notable binding affinities and prime MM/GBSA energies of − 5.04, − 16.07 and − 5.79, − 14.90 kcal/mol, respectively, compared to the reference compound Clomiphene (–7.59, − 14.62 kcal/mol). Molecular dynamics (MD) simulations further validated the enhanced stability of the Chlorpropamide and Tolazamide complexes over the apo form and the reference compound, supported by RMSD, RMSF, RoG, SASA, PCA, and DCCM analyses. Post-MD MM/GBSA binding energy calculations confirmed favorable interactions, with Chlorpropamide and Tolazamide showing − 37.03 ± 3.55 and − 27.82 ± 3.40 kcal/mol, respectively, while Clomiphene showed − 45.16 ± 5.96 kcal/mol. Furthermore, ADME profiling using SwissADME revealed that both Chlorpropamide and Tolazamide possess favorable pharmacokinetic and drug-likeness properties, including high gastrointestinal absorption, good bioavailability scores, and compliance with major drug-likeness filters, supporting their potential as viable therapeutic agents. These results highlight the potential of Chlorpropamide and Tolazamide as promising therapeutic agents for PCOS management.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145256648","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Grosvenorine (Monk Fruit flavonoid) Attenuates Indomethacin-mediated Gastropathy in Vivo: Role of P53/Bcl-2, Antioxidant, and Inflammatory Mediators","authors":"Khaled Abdul-Aziz Ahmed,&nbsp;Khalid M. Alqaisi,&nbsp;Ahmed A.j. Jabbar,&nbsp;Parween Abdulsamad Ismail,&nbsp;Noralhuda Ayad Ibrahim,&nbsp;Hanan Ibrahim Althagbi,&nbsp;Rawaz Rizgar Hassan,&nbsp;Muzhda Haydar Saber,&nbsp;Goran Noori Saleh,&nbsp;Musher Ismail saleh,&nbsp;Talal Salem Alqaisi,&nbsp;Ahmed Hameed Al-Dabhawi","doi":"10.1007/s12247-025-10115-3","DOIUrl":"10.1007/s12247-025-10115-3","url":null,"abstract":"<div><p>Natural products have gained renewed interest as therapeutic agents due to their safer effects compared to medicinal therapeutics. As a major flavonoid of <i>Siraitia grosvenorii</i>, Grosvenorine (GVN) has been used for many health purposes. The present study was geared to unveil the marginal safety dosage and gastroprotective potential of GVN in indomethacin-provoked gastropathy in rats. Thirty Sprague-Dawley rats were arbitrarily grouped and pre-treated with either normal saline (groups A and B), 20 mg/kg omeprazole (C), 30 mg/kg GVN (D), or 60 mg/kg GVN (E). Rats in groups B-E received indomethacin (30 mg/kg) and were euthanized for the histopathological and biochemical investigations. Oral delivery of GVN (250 and 500 mg/kg) did not cause any noticeable toxic signs even after a two-week trial. Pretreatment with GVN (30 and 60 mg/kg) significantly inhibited indomethacin-mediated gastric lesion incidence by 69.03% and 74.89%, respectively. The GVN attenuated gastric histological changes (lowered hemorrhagic/lesion areas and gastric tissue disruptions) and strengthened gastric defensive components (mucin/glycoprotein secretion and gastric pH). GVN pretreatment down-regulated apoptotic rates (increased Bcl-2 and lowered P53 proteins) and significantly heightened antioxidant markers (increased glutathione peroxidase, catalase, and superoxide dismutase contents) in gastric tissues exposed to indomethacin-ulceration. The indomethacin-induced lipid peroxidation (MDA) and inflammatory mediators (TNF-α, interleukin-6) were significantly lower in GVN-treated rats, denoting a preserved gastric homeostatic environment. These outcomes demonstrate that GVN exhibits increased gastroprotective potentials via modulation of apoptosis, antioxidant, and inflammatory mediators, making it a viable source for biopharmaceutical/nutraceutical production.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145256647","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Continuous Manufacturing of Diclofenac Sodium Oleogel Using Co-Rotating Twin Screw Process: Formulation Development and Performance Assessment","authors":"Prerana D Navti,&nbsp;Muralidhar Pisay,&nbsp;Naitik jain,&nbsp;Rahul Pokale,&nbsp;Sanjay Kulkarni,&nbsp;Rakshith Shetty,&nbsp;Krishnaraj Somayaji Shirur,&nbsp;Kunnatur Balasundara Koteshwara,&nbsp;Srinivas Mutalik","doi":"10.1007/s12247-025-10151-z","DOIUrl":"10.1007/s12247-025-10151-z","url":null,"abstract":"<div><h3>Purpose</h3><p>This study focused on the development and optimization of a topical diclofenac sodium oleogel using twin-screw processing (TSP), a continuous manufacturing technology, to overcome limitations of conventional topical formulations. The primary objective was to enhance drug permeation and anti-inflammatory efficacy while enabling scalable, efficient production.</p><h3>Methods</h3><p>A Box-Behnken Design was employed to optimize processing parameters and lecithin concentration. The oleogel was evaluated for yield, organoleptic properties, homogeneity, texture, viscosity, spreadability, pH, drug content, and in vitro drug release. Advanced characterization techniques included X-ray diffraction (XRD), differential scanning calorimetry (DSC). Preclinical studies assessed skin permeation, irritation potential, and pharmacodynamic effects in vivo, alongside biomarker analysis (TNF-α, IL-6, NFκB p65).</p><h3>Results</h3><p>The optimized formulation (DOE-TSP-O) exhibited excellent physical attributes, high drug content, and sustained drug release. XRD and DSC analyses confirmed the amorphous nature and compatibility of components. No skin irritation was observed. In vivo studies demonstrated significantly enhanced analgesic and anti-inflammatory effects compared to conventional hydrogels, with marked reductions in TNF-α, IL-6, and NFκB p65 expression. The formulation remained stable for over three months under long-term storage conditions (25 ± 2 °C, 60% ± 5% RH).</p><h3>Conclusion</h3><p>The DOE-TSP-O formulation represents a promising next-generation topical therapeutic for pain and inflammation, offering superior efficacy and stability. Twin-screw processing enabled scalable, reproducible production, making this a viable approach for advanced topical drug delivery systems.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145256159","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Enhancement of Lurasidone Hydrochloride Dissolution and Pharmacodynamic Properties Via Co-crystal and Eutectic Formation","authors":"Maysa A. Hussien,&nbsp;Sally E. Abu-Risha,&nbsp;Ebtessam A. Essa,&nbsp;Gamal M. El Maghraby,&nbsp;Shimaa M. Ashmawy","doi":"10.1007/s12247-025-10129-x","DOIUrl":"10.1007/s12247-025-10129-x","url":null,"abstract":"<div><h3>Purpose</h3><p>Lurasidone hydrochloride (HCl) is an atypical antipsychotic used for bipolar depression. However, as a Biopharmaceutics Classification System (BCS) Class II drug, it has low solubility, leading to limited oral bioavailability. This study aimed to enhance the dissolution rate and bioavailability of lurasidone HCl by modifying its crystalline structure through co-processing with weak acidic compounds, namely citric acid and nicotinic acid.</p><h3>Methods</h3><p>Lurasidone HCl was co-processed with excipients using the wet co-grinding technique at different molar ratios. The prepared formulations were characterized by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), and X-ray powder diffraction (XRD) to investigate solid-state modifications. Dissolution studies were conducted to evaluate the impact of co-processing on drug release. The optimum ratio for each co-former was selected for in vivo assessment of oral bioavailability using the forced swim test (FST) to evaluate antidepressant activity.</p><h3>Results</h3><p>DSC, FTIR, and XRD confirmed the formation of a lurasidone HCl-citric acid co-crystal, while a eutectic mixture was proposed for lurasidone HCl-nicotinic acid formulations. Dissolution studies demonstrated a two-fold increase in dissolution efficiency compared to unprocessed lurasidone HCl. FST evaluation showed increased immobility durations of 1.7-fold for raw lurasidone HCl, 2.9-fold for the marketed product (Elbaluran^®), 2.19-fold for the co-crystal formulation (F3), and 3.08-fold for the eutectic mixture formulation (F7), respectively.</p><h3>Conclusion</h3><p>Citric acid and nicotinic acid effectively enhanced lurasidone HCl dissolution and bioavailability through co-crystallization and eutectic formation, respectively, offering a promising approach for optimizing its therapeutic efficacy.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s12247-025-10129-x.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145256163","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation of Ferric metal-organic Frameworks Stabilized Sea Buckthorn oil-based Silymarin Incorporated Pickering Nanoemulsion for Oral Squamous Cell Carcinoma Treatment","authors":"Prasad Rodge,&nbsp;Sanjaykumar Bari,&nbsp;Sopan Nangare","doi":"10.1007/s12247-025-10164-8","DOIUrl":"10.1007/s12247-025-10164-8","url":null,"abstract":"<div><p>Oral squamous cell carcinoma (OSCC) is the sixth most common cancer globally, accounting for approximately 90% of all oral malignancies. Ferric-based metal-organic frameworks (Fe-BTC MOFs) have emerged as promising biomaterials due to their tunable surface properties, biocompatibility, and multifunctional applications in drug delivery, including customized release, intrinsic fluorescence, and ferroptosis induction. Silymarin (SL), a natural anticancer compound, exhibits therapeutic potential against oral cancer, while sea buckthorn (SB) oil serves as an effective lipid carrier for hydrophobic drugs. However, the poor aqueous solubility of SL limits its clinical efficacy. To overcome this challenge, we developed a Fe-BTC MOF-stabilized Pickering nanoemulsion (Fe-SB-SL-P-NEmul) for enhanced topical delivery in oral cavity anticancer therapy. The optimized Fe-SB-SL-P-NEmul exhibited excellent colloidal stability, with a zeta potential of -27.58 ± 2.24 mV and a nanometric particle size of 273.3 ± 9.5 nm. Comprehensive characterization through spectral, thermal, and morphological analyses confirmed successful drug encapsulation with high entrapment efficiency (92.69 ± 0.98%) and drug content (98.56 ± 0.87%). In vitro release studies demonstrated sustained drug release, with 92.12 ± 0.97% of SL released over 24 h at pH 6.8, following a diffusion-controlled mechanism. Additionally, the formulation exhibited significant anticancer activity against SCC-9 OSCC cells, likely due to the synergistic effects of SL, SB oil, and Fe-BTC MOFs-induced ferroptosis. Biocompatibility assessments further supported its safety profile. In conclusion, Fe-SB-SL-P-NEmul represents a novel, stable, and efficient nanocarrier system for the targeted delivery of SL in oral cancer therapy. Its ability to enhance drug solubility, modified release, and induce ferroptosis positions it as a promising candidate for future pharmaceutical applications.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145256158","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"RP-HPLC Analysis of Nicotine Content in Diverse Smokeless Tobacco Matrices: A Comparative Study of Commercial and Local Products from India","authors":"Ashu Rathi,&nbsp;Arbab Husain,&nbsp;Afreen Khanam,&nbsp;Mohd Farhan,&nbsp;Mohammad Aatif,&nbsp;Rajeev Singh Raghuvanshi,&nbsp;Gaurav Pratap Singh,&nbsp;Anirudh Malik","doi":"10.1007/s12247-025-10107-3","DOIUrl":"10.1007/s12247-025-10107-3","url":null,"abstract":"<div><h3>Objective</h3><p>The rapid proliferation of smokeless tobacco (SLT) products in India has occurred without sufficient awareness of their toxicological risks and addiction potential. This study developed and validated a robust reversed-phase high-performance liquid chromatography (RP-HPLC) method for the accurate quantification of nicotine in smokeless tobacco products (SLT) includes Tobacco, Snus, Pan masala, Zarda and Supari. The method was optimized for simplicity, accuracy, stability, and rapid analysis, enabling precise determination of nicotine concentrations at microgram-per-gram (ppm) levels. Diverse commercial and locally sourced smokeless tobacco samples from five Indian states (Uttar Pradesh, West Bengal, Hyderabad, Assam and Gujrat) were analysed.</p><h3>Method</h3><p>Optimal chromatographic separation was achieved using an Inertsil C18 column with an isocratic mobile phase of 1.1% triethylamine (TEA) buffer and acetonitrile (75:25, pH 7.0) at a flow rate of 1.0 mL/min. UV detection was performed at 254 nm. The method was validated according to ICH Q2(R1) guidelines.</p><h3>Results</h3><p>The developed HPLC assay demonstrated a nicotine peak purity of 99.62%. Validation parameters met ICH guidelines, with system, method, and intermediate precision RSD values of 0.03%, 0.18%, and 0.12%, respectively. Mean recovery was 99.18%, and linearity was established over a 2.5–150% range (R² = 0.9993). Nylon and PVDF filters were deemed suitable for nicotine analysis. Methanol diluent stability was confirmed for 20 h for standard solutions and 12 h for test solutions. Forced degradation studies revealed significant nicotine instability under acidic, basic, and oxidative conditions. Analysis of 84 smokeless tobacco samples yielded nicotine concentrations ranging from 24.0 to 55296.8 µg/g in West Bengal, 17.2 to 35778.2 µg/g in Uttar Pradesh, 56.3 to 2239.0 µg/g in Gujarat, 7239.0 to 22768.2 µg/g in Himachal Pradesh, and 52.2 to 27192.0 µg/g in Hyderabad.</p><h3>Conclusion</h3><p>Quantitative analysis of smokeless tobacco products across India revealed substantial inter-product variability in nicotine concentrations. These findings highlight the potential public health risks associated with smokeless tobacco use, particularly concerning the addictive nature of nicotine.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145256404","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Ter-polymeric Cytocompatible Hydrogels Based on Sodium Alginate with Pectin and Acrylic Acid for Controlled Loxoprofen Sodium Oral Delivery; In vitro and In vivo Evaluation","authors":"Samiullah Khan,&nbsp;Abdur Rehman,&nbsp;Syed Faisal Badshah,&nbsp;Muhammad Saad","doi":"10.1007/s12247-025-10133-1","DOIUrl":"10.1007/s12247-025-10133-1","url":null,"abstract":"<div><h3>Purpose</h3><p>Controlled and effective drug delivery remained a significant challenge in oral drug therapy. This study was conducted to design novel stable ter-polymeric hydrogels-based delivery system for controlled and effective Loxoprofen sodium release and in turn to reduce side effects after oral administration.</p><h3>Methods</h3><p>Current study reports the development of novel pH responsive ter-polymeric NaAlg/Pec/PAA hydrogels with varied feed composition synthesized <i>via</i> free radical polymerization technique. Swelling analysis and drug release study was conducted in various phosphate buffer solutions. Pharmacokinetic analysis in rabbit model was conducted to investigate the drug plasma concentrations with time. FTIR and SEM analysis was conducted to explore the structural and morphological investigations of optimized ter-polymeric hydrogels.</p><h3>Results</h3><p>Concluded that ter-polymeric NaAlg/Pec/PAA hydrogels exhibited maximum swelling and drug release in basic pH environment (7.5) owing to ionization of carboxyl (-COOH) groups which makes them excellent drug carriers to colon. It was also found that with increasing polymeric contents and crosslinker, gel fraction and porosity of hydrogels increased. Drug release kinetics showed that ter-polymeric hydrogels followed zero order release with non-fickian mechanism. MTT assay confirmed that developed blank and drug loaded hydrogels are biocompatible and safe for oral administration. In vivo analysis in animal model showed that ter-polymeric hydrogels exhibited controlled drug release (C_max=2298.88 ng/ml) for 72 h in comparison to free Loxoprofen sodium solution (C_max= 2337.50 ng/ml) for 40 min. FTIR analysis confirmed the new ter-polymeric hydrogel structure while SEM analysis showed the porous hydrogel structure.</p><h3>Conclusion</h3><p>It is concluded from results that Loxoprofen sodium adverse effect can be effectively controlled after oral administration <i>via</i> encapsulating in ter-polymeric hydrogels.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145256403","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"IVRT and IVPT of Desonide Lotion and Cream: Correlation with Human Bioequivalence Study","authors":"Jie Feng,&nbsp;Om Sambhaji Shelke,&nbsp;Yao Chen,&nbsp;Zheng Zhang,&nbsp;Xiaoqing Tang,&nbsp;Yijie Zhu","doi":"10.1007/s12247-025-10071-y","DOIUrl":"10.1007/s12247-025-10071-y","url":null,"abstract":"<div><h3>Background</h3><p>Topical bioequivalence (BE) studies are critical for approving affordable generic formulations while ensuring safety and efficacy comparable to branded products. However, traditional clinical endpoint studies for topical formulations are costly, time-consuming, and complex. This study explores an in vitro release testing (IVRT) and an in vitro permeation testing (IVPT). The formulations were further evaluated in a bioequivalence study to establish therapeutic equivalence.</p><h3>Methods</h3><p>The IVRT method was developed and validated using 50% ethanol in pH 4.0 acetate buffer as the receptor medium and a Nylon 66 synthetic membrane, demonstrating linearity, precision, sensitivity, and robustness. The IVPT method utilized porcine skin as a substitute model for human skin and saline solution as receptor media to achieve comparable cumulative permeability and penetration rates between test and reference formulations. The pilot and pivotal skin blanching assay was performed using 18 and 100 subjects, respectively.</p><h3>Results</h3><p>The 90% confidence interval of test and reference formulation for the IVRT was 97.78%~107.1% for lotion and 93.5 ~ 112.8% for cream (75%~133.33%). The test and reference formulation of cream and lotion reached the maximum permeability rate (Jmax) at 24 h, and the T/R ratio was 100.0% for cream and 110.0% for lotion (90% CI with 80–125%0). The T/R ratio of the cumulative permeability for the cream and lotion formulation was 95.2% and 104.5% respectively. The average recoveries after the permeation test for T and R cream formulations were 97.4 ± 7.7% and 101.6 ± 10.5% and for lotion, 88.2 ± 5.1 and 86.8 ± 3.9 respectively. Both IVRT and IVPT results confirmed bioequivalence. Additionally, a skin blanching assay further validated the bioequivalence of the test formulations.</p><h3>Conclusion</h3><p>The findings demonstrate that both formulations exhibit comparable release and permeation characteristics, supporting their bioequivalence in human subjects. This integrated approach highlights the utility of IVRT and IVPT as robust tools for formulation development and in vitro bioequivalence assessment of topical dermatological products.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145210250","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}