Journal of Pharmaceutical Innovation最新文献

{"title":"Promising Alginate-Gelatin Scaffolds Containing 5-Fluorouracil and Reinforced with Zinc-Modified Hydroxyapatite: Cell Attachment and One-Year Stability Study","authors":"Ebtesam W. Elsayed,&nbsp;Maha F. Emam,&nbsp;Ahmed A. El-Ashmawy,&nbsp;Gehan T. El-Bassyouni,&nbsp;Sahar M. Mousa,&nbsp;Ahmed A. F. Soliman,&nbsp;M. El-Manawaty,&nbsp;Laila H. Emara","doi":"10.1007/s12247-025-10032-5","DOIUrl":"10.1007/s12247-025-10032-5","url":null,"abstract":"<div><h3>Purpose</h3><p>The current study evaluated the cell attachment capability and long-term stability of 5<b>-</b>fluorouracil (5-FU) loaded alginate-gelatin scaffolds reinforced with zinc-doped hydroxyapatite (Zn-HA).</p><h3>Methods</h3><p>Zn-HA (2% and 6% Zn) was prepared and evaluated for the crystalline nature, chemical structure, and microstructure of hydroxyapatite (HA). Blank and 5-FU loaded alginate-gelatin-Zn-HA scaffolds were prepared and evaluated in terms of surface area, pore size, pore volume, and morphology using the gas adsorption technique and scanning electron microscopy (SEM). Cell attachment studies were also carried out on normal human cell line. The scaffolds were stored for one year at room temperature and evaluated for any changes in their physico-chemical properties as well as 5-FU release profile.</p><h3>Results</h3><p>The results showed that increasing zinc content decreased HA particle size. The blank scaffolds showed higher surface area, pore volume values, and a less porous structure compared to the drug-loaded ones. The pore size increased after scaffolds soaking in cell-line medium due to the hydrogel-forming materials' biodegradability and drug release. Cell growth on the presoaked drug-loaded scaffolds was improved compared to blank scaffold. XRD, FTIR and 5-FU release profile indicated that the stored scaffolds did not show any physical or chemical changes.</p><h3>Conclusion</h3><p>The prepared scaffolds showed promising results regarding cell attachment capability and long-term stability.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-07-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s12247-025-10032-5.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145164728","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":"An Integrated Computational and Experimental Framework for Investigating Flavonoid-driven Bioenhancement of Curcumin","authors":"Pooja Mallya,&nbsp;Mangala Shenoy K,&nbsp;Dani Lakshman Yarlagadda,&nbsp;Suvarna G Kini,&nbsp;Shaila A Lewis","doi":"10.1007/s12247-025-10042-3","DOIUrl":"10.1007/s12247-025-10042-3","url":null,"abstract":"<div><h3>Purpose</h3><p>Enhancing oral bioavailability remains a key focus in modern medicine. Among various bioenhancers, flavonoid polyphenols show significant promise by inhibiting efflux proteins like P-glycoprotein (P-gp), thereby improving intestinal permeability and systemic drug absorption. This study evaluates the P-gp binding affinity of two flavonoids, Naringin (NRG) and Quercetin (QCT), to explore their potential in enhancing the permeability of the P-gp substrate, Curcumin (CUR).</p><h3>Methods</h3><p>P-gp binding affinities of NRG and QCT were evaluated in silico to identify the optimal co-former for CUR in co-amorphous mixture (CAM). Differential Scanning Calorimetry (DSC) was used to preliminarily select the suitable P-gp inhibitor. The chosen co-former was then evaluated for ex vivo permeability studies.</p><h3>Results</h3><p>NRG demonstrated a more favorable MM-GBSA binding energy to P-gp (-39.76 kcal/mol vs. -35.16 kcal/mol for QCT), suggesting a stronger and more stable interaction overall. Additionally, DSC analysis unveiled the conversion of CUR from a crystalline to an amorphous form when co-formulated with NRG, likely accredited to the glass-forming ability of NRG. In contrast, CAM of CUR with QCT did not induce transformation of crystalline CUR into its amorphous form which could attributed to the formation of poor glass structures within the CAM. To further validate the P-gp inhibition potential of NRG, <i>ex-vivo</i> permeability studies were carried out and the CAM of CUR and NRG in molar ratio 1:2 demonstrated a maximum of 19-fold increase than CUR (P &lt; 0.05). CAM (1:1) and physical mixture displayed 3.8-and 2-folds increase in permeability than CUR, respectively (P &lt; 0.05).</p><h3>Conclusion</h3><p>These study findings are indicative of potential advantage of NRG as a co-former, promising improved oral bioavailability of CUR.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-07-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145165127","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":"Formulation of Mixed Micelles of Various Model Drug Ionic Complexes in an Optimized Micellar Base Composed of Surfactants and Cosolvent Mixture: In Vitro Analysis of Drug Delivery Efficiency","authors":"Ahmad Saleh Malkawi,&nbsp;Collins Ovenseri Airemwen,&nbsp;Azhar Malkawi","doi":"10.1007/s12247-025-10041-4","DOIUrl":"10.1007/s12247-025-10041-4","url":null,"abstract":"<div><h3>Objective</h3><p>In this study, micellar complexes of various model drugs were developed and investigated for drug delivery efficiency.</p><h3>Method</h3><p>Ponceau 4R, captopril, and fluorescein were chosen as model drugs to form ionic complexes with three Eudragit-based polymers (Eudragit RL, RS, and E). The formed model drug complexes were Eudragit RL-ponceau 4R (RLP), Eudragit RS-ponceau 4R (RSP), Eudragit RS-captopril (RSC), Eudragit E-captopril (EC), and Eudragit RS-fluorescein (RSF). RLP, RSP, RSC, EC, and RSF were incorporated into a micellar base composed of 40% Kolliphor RH 40, 20% Kolliphor EL, 15% Capmul MCM, and 25% dipropylene glycol to form MRLP, MRSP, MRSC, MEC, and MRSF micellar complexes, respectively. Micellar complexes were diluted in physiological buffer media (pH 7.4) and characterized regarding the size, polydispersity index (PDI), zeta potential, critical micelle concentration (CMC), and safety on Caco-2 cells. Micellar complex efficiency in model drug delivery was investigated through a drug release study, cellular uptake, and confocal microscopy.</p><h3>Results</h3><p>Micellar complexes preserved a stabilized size (14.38–91.38 nm) with a PDI ≤ 0.3 and exhibited a zeta potential in the range of + 2.21 mV to + 12.23 mV. CMC of all micellar formulations was in the range of 130–230 µg/mL. At 0.5:100, 1:100, 2:100, and 3:100 dilutions, micellar complexes maintained a considerable safety limit, shown as 85–100% cell viability over Caco-2 cells. All micellar complexes were compatible for a sustained drug release with an average of 94.85 ± 1.42% model drug release within 4–6 h. The release pattern of model drugs from the micellar complexes followed First-order kinetics. Comparatively, cellular uptake of model drugs from the micellar complexes was significantly higher as compared to the control of free model drug solutions (p ≤ 0.001). MRLP and MRSP, MRSC and MEC, and MRSF showed 5.7- to 9.4-fold, 2.9- to 4.4-fold, and 4.2-fold higher model drug cellular uptake than ponceau 4R, captopril, and fluorescein as free model drug solutions, respectively. Confocal microscopic imaging showed a remarkable fluorescent intensity as an indication of fluorescein cellular uptake from MRSF.</p><h3>Conclusion</h3><p>The studied micellar complexes provided proof of an efficient drug delivery vehicle by showing a sustained optimum drug release and a significantly enhanced model drug cellular uptake while maintaining adequate biocompatibility.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-07-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145164536","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":"Exploring the Anti-Inflammatory Effects of Grape Seed Extract on Depressive Disorder: A Preclinical and Network Pharmacology Approach","authors":"Marina Rigotti,&nbsp;Laura Ferrazzi Finger,&nbsp;Júlia Maiara dos Santos,&nbsp;Luciana Bavaresco Andrade Touguinha,&nbsp;Adriano Costa De Camargo,&nbsp;Alina Concepción-Alvarez,&nbsp;Raquel Bridi,&nbsp;Michel Mansur Machado,&nbsp;Lucielli Savegnago,&nbsp;Catia Santos Branco","doi":"10.1007/s12247-025-10034-3","DOIUrl":"10.1007/s12247-025-10034-3","url":null,"abstract":"<div><p>Grape seed extract (GSE) is a biotechnological input known for its anti-inflammatory and neuroprotective properties. This study aimed to chemically characterize GSE and evaluate their effects on targets associated with the gut-brain axis in depression using in silico methods. Phenolic bioaccessibility and in vitro and in vivo safety profiles were also assessed. Network pharmacology (NP) was employed to identify the properties and potential targets of GSE’s main bioactive compounds, which were identified via High-Performance Liquid Chromatography with Diode-Array Detection (HPLC-DAD). Molecular docking was performed with target proteins involved in depression-related toll-like receptor (TLR) signaling pathways. The bioaccessibility, antioxidant activity, total polyphenol content of GSE were evaluated across all digestive stages, and BV-2 microglial cells were exposed to the final digestion metabolites. The significant compounds catechin and rutin exhibited molecular affinity with the proteins AKT1 and MAPK8, suggesting an anti-inflammatory effect of GSE. Bioaccessibility assays revealed a reduction of phenolic compounds during the gastric and duodenal digestion phases, which were reestablished to levels like the control in the jejunal and ileal phases. The digested extract (concentrations ≤ 50 µg/mL; 24 h) was non-cytotoxic to BV-2 cells and did not alter the production of nitric oxide (NO) or reactive oxygen species (ROS) (<i>p</i> &gt; 0.05). These results suggest that GSE may be a promising candidate for modulating inflammation-related conditions. Additionally, in vivo toxicity assessments using the <i>Artemia salina</i> model indicated that the extract is safe for in vivo applications.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-07-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145164530","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":"Protection of Mucous Membranes Against the Use of Biocides","authors":"Cristina Alonso Merino,&nbsp;Luisa Coderch,&nbsp;Ana Cristina Calpena,&nbsp;Beatriz Clares,&nbsp;Anderson Ramos,&nbsp;Meritxell Martí","doi":"10.1007/s12247-025-09995-2","DOIUrl":"10.1007/s12247-025-09995-2","url":null,"abstract":"<div><h3>Background</h3><p>Biocides, in touch with the mucosa or skin, are capable of penetrating the mucosa or skin and causing possible local lesions, such as irritations, allergic contact dermatitis and even systemic effects such as carcinogenesis. The high permeability of compounds across the oral or nasal mucosa is widely known, in comparison to the poor penetration across the skin. Therefore, the main objective of this work is to produce a formulation that can strengthen the mucosa, increasing its hindering effect and thus decreasing or avoiding the penetration of contaminants and biocides.</p><h3>Results</h3><p>Several compositions have been formulated and assayed; the hydrophobic formulation F1, the hydrophilic formulation F2 and the liposomal formulations F3 with lipids and structure similar to those present in cutaneous keratinous tissues. These all induced a waterproofing effect with the liposomal formulation F3 and in particular the hydrophobic formulation F1 inducing the greatest decrease in Trans-mucosal water loss. Permeation of the three biocides Fungitrol, Propiconazole and Permethrin was evaluated in skin and in untreated and treated (F1, F2, F3) oral mucosal membranes. The influence of the three formulations on each of the biocides used is considerable, reaching values significantly equal to those of the skin for formulation 1. While hydrophilic formulation 2 greatly increases permeability, hydrophobic formulation 1 and liposomal formulation 3 reduce permeability, in approximately 90% and 60% respectively, providing an almost skin-like barrier effect.</p><h3>Conclusions</h3><p>Therefore, this work presents two formulations that induce mucosal impermeability by reducing the penetration of three model biocides.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s12247-025-09995-2.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145164285","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":"Development of Bimatoprost-Loaded Nano Spanlastic In-Situ Gel for Ophthalmic Drug Delivery: A Box-Behnken Optimization Approach with In Vitro and Ex Vivo Characterization","authors":"Rajashree Masareddy,&nbsp;Pradnya Patted,&nbsp;Archana S. Patil,&nbsp;Krutuja R. Chougule","doi":"10.1007/s12247-025-10031-6","DOIUrl":"10.1007/s12247-025-10031-6","url":null,"abstract":"<div><h3>Purpose</h3><p>The present study aimed to develop and optimize a Bimatoprost-loaded spanlastic in-situ gel to enhance precorneal retention, corneal penetration, and therapeutic efficacy while minimizing ocular side effects.</p><h3>Methods</h3><p>Spanlastic vesicles were prepared using the ethanol injection method and optimized using a 3³ Box-Behnken design. The optimized formulation was characterized for morphology using transmission electron microscopy (TEM), particle size, entrapment efficiency, and drug-excipient compatibility using FTIR and DSC. The in-situ gel was formulated using 18% poloxamer 407 and evaluated for viscosity, gelling capacity, and drug content. Drug release kinetics, ex vivo corneal permeation through goat cornea, and ocular irritation using the HET-CAM assay were assessed. Sterility, isotonicity, and stability studies were also conducted.</p><h3>Results</h3><p>TEM analysis revealed uniform spherical vesicles with a mean particle size of 156.1 ± 0.82 nm. The vesicles demonstrated high entrapment efficiency and compatibility with excipients. The in-situ gel exhibited favourable viscosity of 610 ± 1.09 cps, rapid gelation, and high drug content of 99.52 ± 1.28%. Drug release followed a sustained pattern best described by the Korsmeyer-Peppas model. Ex vivo studies showed enhanced corneal permeation of 89.56% for 8 h, while HET-CAM assays indicated minimal ocular irritation. The optimized formulation (SPs-ISG 18%) was sterile, isotonic, and stable at room temperature.</p><h3>Conclusion</h3><p>The developed Bimatoprost-loaded spanlastic in-situ gel demonstrates promising potential as a safe and effective ocular delivery system for glaucoma management, offering improved corneal penetration and sustained release.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145163227","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":"Phytochemical Composition and Bioactivities of Verbena tenuisecta (Briq.) Leaf Extracts: Antimicrobial and Antibiofilm Properties","authors":"Amna Azeem,&nbsp;Atta Ur Rahman,&nbsp;Arshad Iqbal,&nbsp;Fahmeeda Kausar,&nbsp;Sobia Gul,&nbsp;Atif Ali Khan Khalil,&nbsp;Khalid Rehman Hakeem,&nbsp;Sumaira Noor,&nbsp;Ali Zari,&nbsp;Muskaan Zaman,&nbsp;Khalid M. Alghamdi,&nbsp;Rohin Iqbal Khan,&nbsp;Tanveer Bilal Pirzadah","doi":"10.1007/s12247-025-10018-3","DOIUrl":"10.1007/s12247-025-10018-3","url":null,"abstract":"<div><h3>Background</h3><p>Many plants have been reported to exhibit both antimicrobial and anti-biofilm activities potentially serving as natural alternative to conventional synthetic antimicrobials.</p><h3>Objective</h3><p>In this context, the present study was aimed to evaluate the phytochemical composition and bioactivities of <i>Verbena tenuisecta</i> leaf extracts.</p><h3>Methods</h3><p>Qualitative phytochemical screening was conducted to detect the presence of major phytochemical groups. Gas Chromatography-Mass Spectrometry (GC-MS) analysis was carried out to identify key bioactive compounds. Antimicrobial activities were evaluated using the Well Diffusion Method. Antibiofilm activity was assessed using a microtiter plate-based crystal violet assay.</p><h3>Results</h3><p>Qualitative phytochemical analysis of the crude methanolic extract confirmed the presence of alkaloids, terpenoids, phenols, flavonoids, glycosides, and carbohydrates. GC–MS analysis of the chloroform fraction identified seven bioactive compounds with Phenyton, Benzoyl oleic acid, Indole,6-methyl-2-(4-pyridyl)- as major components. Antibacterial activity revealed that the crude methanolic extract exhibited the highest zones of inhibition (ZOI) (13.25 mm) against <i>Bacillus subtilis</i> while showed moderate activity against <i>Escherichia coli</i> (11.75 mm), <i>Salmonella typhi</i> (11.25 mm) and <i>Staphylococcus aureus</i> (11.5 mm). Among the fractions subjected, the n-hexane and chloroform fractions displayed notable antibacterial effects, with ZOI values compared to standard antibiotic. Antifungal activity of Chloroform extracted sample showed highest inhibitory effect against <i>Candida albicans</i> with ZOI of 15.25 mm as compared to extracts. Antibiofilm assay revealed varying inhibitory potential of different extracts tested. Crude methanolic extract showed the highest inhibition against <i>E. coli</i> (1.746) and <i>Staphylococcus aureus</i> (1.133). Similarly, n-butanol fraction exhibited significant antibiofilm activity against <i>Staphylococcus aureus</i> (1.733), while the chloroform fraction showed moderate anti-biofilm activity.</p><h3>Conclusion</h3><p>These findings highlight the potential of <i>V. tenuisecta</i> as a source of bioactive compounds with antibacterial, antifungal, and antibiofilm properties. Further research work is warranted to isolate and characterize the bioactive compounds of <i>Verbena tenuisecta</i> as lead antimicrobial agents.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-07-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145163231","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":"Formulation, In Vitro Characterization and Anti-Tuberculosis Investigation of Isoniazid NANOCAPSULES.","authors":"Chekwube A. Ezegbe,&nbsp;Chukwuemeka C. Mbah,&nbsp;Amarachi G. Ezegbe,&nbsp;Ifeanyi S. Ofoefule,&nbsp;EZINNE C. OKORAFOR","doi":"10.1007/s12247-025-10030-7","DOIUrl":"10.1007/s12247-025-10030-7","url":null,"abstract":"<div><h3>Purpose</h3><p>Tuberculosis (TB) is a major cause of mortality worldwide. The most commonly used first-line anti-TB drugs in the treatment of TB are rifampicin and isoniazid. This research aimed to formulate and evaluate the anti-mycobacterium activity of isoniazid (INH) nano capsules against mycobacterium isolates (<i>M. smegmatis</i> and <i>M. bovis</i>).</p><h3>Methods</h3><p>Lecithin was extracted from locally sourced soybean (<i>Glycine max</i>) by aqueous degumming method. Nanoparticles of INH were prepared by mechanical dispersion method. Chitosan was dispersed in 100 mL of acetic acid solution in distilled water overnight. Sodium tripolyphosphate (STPP) was dissolved in 10 mL of distilled water, and added to the chitosan dispersion and stirred using magnetic stirrer at 100 rpm for 30 min. The chitosan/STPP solution and Labrasol® (0.2%), was then added to the organic solution in drops using a syringe and stirred at 10,000 rpm for 45 min using Ultra-turax homogenizer. Subsequently, the precipitate formed was collected after 3 h by centrifugation at 4000 rpm<i>.</i> Nanoparticles obtained were adsorbed by mixing with Neusilin® (0.5%) to form powdered products. Preformulation studies were done using Fourier Transform Infra-Red (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC) and Design Expert®. The nano formulations were characterized for particle size using zeta sizer, morphology by scanning electron microscopy (SEM), thermal properties, entrapment efficiency (EE) and in vitro release.</p><h3>Results</h3><p>The percentage yield of the extracted lecithin ranged from 31.0 ± 0.31% to 35.0 ± 0.32%. The DSC thermograph of pure INH was 168.0 °C. The drug content of INH formulation with extracted lecithin (IEL) and isoniazid formulation with reference lecithin (IRL) ranged from 96.4 ± 0.29% to 93.5 ± 0.94% respectively. Encapsulation efficiency for both IEL and IRL were 95.40 ± 0.37% and 95.70 ± 0.10% respectively. INH nano capsule formulations showed significantly (<i>p</i> &lt; 0.05) lower MICs (0.03 μg/mL) than the reference commercial nano capsule (0.05 and 0.10 μg/mL) against <i>M. smegmatis</i> and <i>M. bovis</i> isolates, respectively.</p><h3>Conclusion</h3><p>The mycobacterium assay verified that the INH nano capsules had higher potential of activity against the mycobacterial isolates than the conventional nanocapsules. The higher activity may be attributed to increased permeation of the bacterial cell wall, because Labrasol® was used as a permeation enhancer.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145162453","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":"Development and Pharmacokinetic Evaluation of Binary Carrier-Based Solid Dispersion of Desidustat, a New Drug for Chronic Kidney Disease-Associated Anemia","authors":"Dekai Banerjee,&nbsp;Sanjay Sharma,&nbsp;Bappaditya Chatterjee","doi":"10.1007/s12247-025-10000-z","DOIUrl":"10.1007/s12247-025-10000-z","url":null,"abstract":"<div><h3>Purpose</h3><p>Desidustat is a new oral hypoxia-inducible factor prolyl hydroxylase inhibitor indicated for the management of chronic kidney disease-related renal anemia. Poor aqueous solubility of desidustat restricts its dissolution and leads to poor oral bioavailability.</p><h3>Methods</h3><p>A simple melt quenching method has been developed for solid dispersions (SD) of desidustat using PVP K30 and poloxamer 188 as a binary carrier system. Polymer selection was done based on the miscibility study with the drug.</p><h3>Results</h3><p>The aqueous solubility of desidustat was increased up to 8 times in SD with a drug: carrier (PVPK30-poloxamer 188) ratio of 1:3 (w/w). Thermal analysis by DSC indicated conversion of crystalline desidustat to amorphous in solid dispersion. Hydrogen bonding between the drug and polymer was noticed by infrared (IR) spectroscopy. Powdered X-ray diffraction revealed the loss of crystalline drug peaks in SD, confirming its conversion from crystalline to partially amorphous. An in vitro drug release study showed 96.8% release from desidustat SD in 6 hours in a basic medium (pH 6.8). The enhancement of dissolution was dependent on the drug: carrier ratio. The increased solubility by the hydrophilic carrier system and the loss of crystallinity are two main reasons for enhanced dissolution. An in vivo pharmacokinetic study showed 1.6 times enhancement in oral bioavailability from desidustat solid dispersion compared to the raw drug.</p><h3>Conclusion</h3><p>The solid dispersion approach can improve desidustat oral bioavailability. PVP K30 and poloxamer 188 can serve as an effective binary carrier system for the dispersion.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145161969","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":"“Therapeutic Potential of Boswellic Acid-Loaded Nanostructured Lipid Carriers in Aloe Gel: A Novel Approach for Effective Gout Management on Wistar Rats”","authors":"Sahil Naik,&nbsp;Kishori P. Sutar,&nbsp;Sankalp S. Sammasagi,&nbsp;Prakash Biradar,&nbsp;Anvitha Sequeira,&nbsp;Arun Jadhav","doi":"10.1007/s12247-025-10023-6","DOIUrl":"10.1007/s12247-025-10023-6","url":null,"abstract":"<div><h3>Purpose</h3><p>The present study aims to develop, optimize, and evaluate 3-acetyl-11-keto-ꞵ-Boswellic acid-loaded nanostructured lipid carriers incorporated into an aloe-based gel for effective gout management. The objective was to enhance drug permeation, achieve sustained release, and overcome challenges associated with oral delivery of 3-acetyl-11-keto-ꞵ-Boswellic acid.</p><h3>Methods</h3><p>Nanostructured lipid carriers were prepared using the micro-emulsion method, employing a Box-Behnken full factorial design with varying concentrations of stearic acid, oleic acid, and Tween 80. Optimization was based on particle size, zeta potential, entrapment efficiency, Polydispersibility Index, drug content, and in vitro release. Transmission electron microscopy confirmed the nano-sized, well-dispersed particles. The optimized batch (F5) was incorporated into a 1.5% w/v aloe-based gel, which was subsequently assessed for pH, viscosity, spreadability, in vitro diffusion, in vivo dermal irritancy, and efficacy against Monosodium Urate-induced gout.</p><h3>Results</h3><p>The optimized Nanostructured lipid carriers exhibited a particle size of 110.1 nm, zeta potential of -32.1 mV, entrapment efficiency of 80.3%, and drug content of 78.21 ± 1.57%. The gel formulation showed a viscosity of 781 ± 6.16 cps, spreadability of 7.67 ± 0.0942 g.cm/sec, and pH of 6.24 ± 0.05. In vitro drug release was 85.96% over 12 h, with the gel demonstrating 83.01% diffusion. In vivo studies confirmed significant therapeutic efficacy, non-irritancy, and enhanced mobility in treated subjects.</p><h3>Conclusion</h3><p>The boswellic acid-loaded Nanostructured lipid carriers aloe gel offers a promising strategy for gout management, providing enhanced permeation, sustained release, and minimal dermal irritation. Stability studies further support its potential for therapeutic application.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145161260","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}