Pharmaceutical Development and Technology最新文献

Investigating the effect of leucine and dipalmitoylphosphatidylcholine on aerosolization properties of high-dose dry powder inhaler formulations of itraconazole nanoparticles. 研究亮氨酸和双棕榈酰磷脂酰胆碱对伊曲康唑纳米颗粒大剂量干粉吸入剂雾化性能的影响。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-10-19 DOI: 10.1080/10837450.2026.2746980

Peyman Khoshhal, Mohammadreza Rouini, Kambiz Gilani

{"title":"Investigating the effect of leucine and dipalmitoylphosphatidylcholine on aerosolization properties of high-dose dry powder inhaler formulations of itraconazole nanoparticles.","authors":"Peyman Khoshhal, Mohammadreza Rouini, Kambiz Gilani","doi":"10.1080/10837450.2026.2746980","DOIUrl":"10.1080/10837450.2026.2746980","url":null,"abstract":"This study aims to develop a high-dose dry powder inhaler (DPI) formulation of itraconazole (ITZ) nanoparticles with leucine and/or dipalmitoylphosphatidylcholine (DPPC) as excipients to increase drug solubility and aerosolization performance. To do this, we co-spray-dried leucine and DPPC with an optimized ITZ nanosuspension and measured the physical properties, dissolution and aerosolization characteristics of the formulations. Among the formulations, those containing 50% (w/wITZ) leucine (N3) or 30% (w/wITZ) leucine with 20% (w/wITZ) DPPC (N5), which had the highest FPF (68.88 ± 1.90% for N3 and 78.81 ± 1.17% for N5) and dissolved percentage of the drug (cumulative release percentage in 180 min, 69.10 ± 1.46% for N3 and 94.34 ± 1.30% for N5), were selected for in vivo pharmacokinetic studies and insufflated intratracheally to rats. An ITZ suspension was administered as a control by gavage. Among the selected formulations, N3 produced the highest AUC in lung tissue, approximately two-fold higher than N5. Furthermore, the AUCLung-to-AUCPlasma ratio for N3 was approximately 24-fold and 800-fold higher than those of N5 and the oral formulations, respectively, indicating enhanced pulmonary retention and potentially reduced systemic exposure. Overall, N3 represents a promising high-dose DPI formulation for further preclinical development of inhaled ITZ.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-18"},"PeriodicalIF":2.9,"publicationDate":"2026-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149168583","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}

引用次数: 0

Chitosan-modulated niosomes for improved ocular delivery of brinzolamide. 壳聚糖调节乳小体改善溴唑胺眼部递送。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-10-13 DOI: 10.1080/10837450.2026.2744195

Marina K Sobhy, Abdelaziz E Abdelaziz, Eman A Mazyed, Ahmed A A Youssef, Aya R Elbasuony, Gamal M El Maghraby

{"title":"Chitosan-modulated niosomes for improved ocular delivery of brinzolamide.","authors":"Marina K Sobhy, Abdelaziz E Abdelaziz, Eman A Mazyed, Ahmed A A Youssef, Aya R Elbasuony, Gamal M El Maghraby","doi":"10.1080/10837450.2026.2744195","DOIUrl":"10.1080/10837450.2026.2744195","url":null,"abstract":"Brinzolamide (BZ) is considered a promising pharmaceutical agent for lowering elevated intraocular pressure (IOP). However, its poor aqueous solubility limits its ocular bioavailability. Niosomes showed promising potential in ophthalmic delivery. Chitosan coating may extend the benefits of niosomes by imparting mucoadhesive potential. The aim of this investigation was to explore the potential of chitosan-coated niosomes (CS-niosomes) for improving the ocular delivery of BZ. Standard niosomes composed of Span 60, cholesterol, and ursodeoxycholic acid were loaded with BZ. The same system was coated with chitosan to provide CS-niosomes. Niosomes morphology, size, BZ entrapment efficiency and release were determined. The IOP-lowering effect of BZ-loaded niosomes was monitored after ocular administration in rabbits with experimentally induced glaucoma using lab-prepared suspension and marketed eye drops (Azopt®) as control. Standard niosomes and CS-niosomes were spherical vesicles having size of 193.50 and 159.90 nm, respectively. BZ was entrapped with efficiency of 90.02% and 88.43% in both systems, respectively, with no significant difference observed in their release behaviour. With respect to IOP-lowering ability, CS-niosomes > standard niosomes > Azopt® > lab-prepared suspension with CS-niosomes preserving the efficacy even after 10 h. This study demonstrated the potential of CS-niosomes as a promising nanocarrier for enhanced ocular delivery of BZ.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-13"},"PeriodicalIF":2.9,"publicationDate":"2026-10-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149113564","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}

引用次数: 0

Topical kojic acid liposomes for alkali-induced corneal injury: comparative study of uncoated vs. hyaluronic acid-coated formulations in corneal epithelial repair. 外用曲酸脂质体治疗碱性角膜损伤：未包被与透明质酸包被配方在角膜上皮修复中的比较研究。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-10-10 DOI: 10.1080/10837450.2026.2744579

Menna Mohy Eldeen, Mai Rady, Mohammad Abdel-Halim, Samar Mansour

{"title":"Topical kojic acid liposomes for alkali-induced corneal injury: comparative study of uncoated vs. hyaluronic acid-coated formulations in corneal epithelial repair.","authors":"Menna Mohy Eldeen, Mai Rady, Mohammad Abdel-Halim, Samar Mansour","doi":"10.1080/10837450.2026.2744579","DOIUrl":"10.1080/10837450.2026.2744579","url":null,"abstract":"Corneal chemical injuries are ocular emergencies that can progress to severe ulceration, scarring, and vision loss. This study evaluated topically delivered kojic acid (KA), an agent known for cell proliferation and anti-inflammatory properties in an alkali-induced corneal injury model. Uncoated liposomes and HA coated liposomes were investigated to deliver KA in the corneal tissue. Small (∼200 nm; SL-KA, SL-KA-HA) and large (∼500 nm; LL-KA, LL-KA-HA) liposomes and HA coated liposomes were formulated. Larger liposomes either coated or uncoated exhibited superior ex vivo corneal retention compared to smaller nanocarriers, with uncoated large liposomes (LL-KA: 0.613 ± 0.02 µg) achieving higher retention than HA-coated liposomes (LL-KA-HA: 0.372 ± 0.04 µg). In a 21-day rabbit model of alkali-induced corneal injury, untreated controls showed persistent inflammation and cellular adhesion, whereas free KA failed to alleviate necrosis. Conversely, LL-KA and LL-KA-HA significantly enhanced structural healing, preserved intact epithelia, and reduced stromal alterations, with superior tissue recovery in the LL-KA group. HA solution controls preserved the epithelium but failed to resolve underlying stromal inflammation. Immunohistochemistry demonstrated a marked reduction in NF-κB expression in liposome-treated groups compared to untreated, free KA, or HA controls. Liposomal delivery of KA offers a promising non-surgical therapy for alkali-induced corneal injuries, with uncoated large liposomes emerged better corneal healing.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-14"},"PeriodicalIF":2.9,"publicationDate":"2026-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149113566","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}

引用次数: 0

Nanostructured mucoadhesive buccal tablets for apixaban delivery: mechanistic insights into transmucosal transport and systemic bioavailability. 用于阿哌沙班给药的纳米结构黏附口腔片：通过粘膜转运和全身生物利用度的机制见解。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-10-09 DOI: 10.1080/10837450.2026.2744568

Dalia A Gaber

{"title":"Nanostructured mucoadhesive buccal tablets for apixaban delivery: mechanistic insights into transmucosal transport and systemic bioavailability.","authors":"Dalia A Gaber","doi":"10.1080/10837450.2026.2744568","DOIUrl":"10.1080/10837450.2026.2744568","url":null,"abstract":"This study developed and evaluated a nanoparticle-in-matrix mucoadhesive buccal delivery system for apixaban (APX) to improve its dissolution and systemic exposure. APX-loaded polymeric nanoparticles were prepared by antisolvent nanoprecipitation and incorporated into thiolated chitosan-Carbopol® buccal matrices by direct compression. The optimized nanoparticles exhibited a diameter of 195 ± 22 nm and a 6-fold increase in saturated solubility. The optimized tablets showed rapid hydration (55 ± 4 s), strong mucoadhesion, prolonged ex vivo mucosal retention (7.84 ± 0.41 h), and approximately 80% drug release within 10 min. Ex vivo studies demonstrated a mucosal penetration depth of 285 ± 18 μm. In rabbits, the optimized buccal formulation significantly increased Cmax (3950 ± 310 ng/mL) and AUC0-24 (31,600 ± 2850 ng·h/mL) compared with marketed tablets (420 ± 55 ng/mL and 4120 ± 390 ng·h/mL, respectively), representing approximately 9.4-fold and 7.7-fold higher exposure (p < 0.05). Faster systemic absorption was also observed, with a Tmax of 0.75 ± 0.20 h and Ka of 1.48 ± 0.18 h-1. Changes in PT and aPTT were observed; however, these conventional assays have limited sensitivity for quantitatively assessing apixaban pharmacodynamic activity. Histopathological examination indicated favorable local tissue compatibility. Overall, the nanoparticle-in-matrix buccal system markedly enhanced and accelerated APX exposure in rabbits, supporting its potential for buccal delivery while emphasizing the need for dose optimization, pharmacodynamic assessment, and dedicated safety evaluation before clinical translation.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-22"},"PeriodicalIF":2.9,"publicationDate":"2026-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149128228","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}

引用次数: 0

Mucoadhesive tacrolimus formulations for buccal application: a formulation and drug delivery feasibility study for oral lichen planus. 口腔黏附他克莫司制剂：口腔扁平苔藓的制剂及给药可行性研究。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-10-06 DOI: 10.1080/10837450.2026.2738760

Alexander Hoffreiter, Emily Graf, Dominique Jasmin Lunter

{"title":"Mucoadhesive tacrolimus formulations for buccal application: a formulation and drug delivery feasibility study for oral lichen planus.","authors":"Alexander Hoffreiter, Emily Graf, Dominique Jasmin Lunter","doi":"10.1080/10837450.2026.2738760","DOIUrl":"10.1080/10837450.2026.2738760","url":null,"abstract":"Tacrolimus is a potent calcineurin inhibitor suitable for the local treatment of oral mucosal immune-mediated diseases; however, no buccal formulation is currently available. The main objective of this work was to develop a mucoadhesive, semi-solid formulation containing tacrolimus that has adequate mucoadhesion salivation, and effective mucosal penetration with low systemic availability. A series of tacrolimus containing semisolid formulations based on chitosan, carbomer and hypromellose (HPMC) as mucoadhesive polymers were developed. Their rheologic behavior, pH value, macroscopic and microscopic properties as well as mucoadhesion and mucosal penetration were investigated. Lactate buffer was successfully used to stabilize chitosan against hydrolysis. It was shown that diols of different chain length, like 1,2-propanediol 1,2-pentanediol and 1,2-hexanediol improved mucosal penetration but reduced mucoadhesion due to gel matrix weakening. After 60 min in the mucoadhesion cell, mucosal tacrolimus amounts versus salivary wash-off for the diols were 0.78 ± 0.09 µg/cm2 versus 0.47 ± 0.20% for 20% 1,2-propanediol, 1.99 ± 0.23 µg/cm2 versus 14.26 ± 3.01% for 40% 1,2-propanediol, 3.56 ± 0.29 µg/cm2 versus 25.04 ± 1.68% for 20% 1,2-pentanediol, and 3.66 ± 0.25 µg/cm2 versus 28.13 ± 4.00% for 20% 1,2-hexanediol. A series of tacrolimus formulations with different degrees of mucoadhesion, salivary retention and penetration characteristics was successfully developed.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-24"},"PeriodicalIF":2.9,"publicationDate":"2026-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149039967","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}

引用次数: 0

Development and optimisation using D-optimal design of dual-functionalized hyaluronic acid-chitosan-coated mesoporous silica nanoparticles for repurposed propranolol delivery in breast cancer: a proof-of-concept study. 开发和优化双功能化透明质酸-壳聚糖包被介孔二氧化硅纳米颗粒用于乳腺癌重新用途的心得安输送：一项概念验证研究。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-10-02 DOI: 10.1080/10837450.2026.2738747

Mervat Shafik Ibrahim, Nihal Mohamed Elmahdy Elsayyad, Shereen H Noshi

{"title":"Development and optimisation using D-optimal design of dual-functionalized hyaluronic acid-chitosan-coated mesoporous silica nanoparticles for repurposed propranolol delivery in breast cancer: a proof-of-concept study.","authors":"Mervat Shafik Ibrahim, Nihal Mohamed Elmahdy Elsayyad, Shereen H Noshi","doi":"10.1080/10837450.2026.2738747","DOIUrl":"10.1080/10837450.2026.2738747","url":null,"abstract":"Drug repurposing combined with nanocarrier systems can accelerate cancer therapy development while reducing the time and cost of conventional drug discovery. We developed and optimised hyaluronic acid (HA)-chitosan (CH)-coated mesoporous silica nanoparticles (HA-CH-Prop-MSNPs) for delivery of the repurposed β-blocker propranolol. A two-stage D-optimal design optimised propranolol loading, then CH and HA coating, using particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency (EE). The formulation (0.2% low-molecular-weight CH, 0.07% HA, 2 mg/mL propranolol, 10 mg/mL mesoporous silica nanoparticles) exhibited a particle size of 200.5 nm, PDI of 0.495, zeta potential of -25.7 mV, and EE of 91.2%. HA-CH coating provided controlled release and shifted the mechanism from near-Fickian diffusion toward an increasing contribution from polymer relaxation-controlled transport. Propranolol release was significantly higher at tumour-mimicking pH 5.5 than at physiological pH 7.4 across all formulations. Compared with free propranolol, HA-CH-Prop-MSNPs reduced the IC50 against MCF-7 breast cancer cells 2.8-fold while maintaining negligible carrier cytotoxicity. Under accelerated storage conditions (40 °C/75% RH), the formulation remained stable for six months, with less than a 2% reduction in EE. These findings provide proof of concept that HA-CH-coated mesoporous silica nanoparticles enhance the in vitro anticancer activity of repurposed propranolol through encapsulation and controlled release, laying the foundation for future investigation of HA-mediated cellular targeting.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-20"},"PeriodicalIF":2.9,"publicationDate":"2026-10-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149030962","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}

引用次数: 0

Preparation and in vitro evaluation of amphotericin B-chondroitin sulfate polymer prodrug. 两性霉素b -硫酸软骨素聚合物前药的制备及体外评价。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-29 DOI: 10.1080/10837450.2026.2740069

Jingqiu Sun, Qingyun Yu, Weijun Chen, Lingtong Ge, Anran Jiao, Haoxin Ding, Lipeng Qiu, Qingfeng Guo

{"title":"Preparation and in vitro evaluation of amphotericin B-chondroitin sulfate polymer prodrug.","authors":"Jingqiu Sun, Qingyun Yu, Weijun Chen, Lingtong Ge, Anran Jiao, Haoxin Ding, Lipeng Qiu, Qingfeng Guo","doi":"10.1080/10837450.2026.2740069","DOIUrl":"10.1080/10837450.2026.2740069","url":null,"abstract":"Amphotericin B (AmB) remains the gold-standard antifungal agent, yet its clinical utility is severely limited by dose-dependent hemolytic and nephrotoxic side effects arising from its aggregation-prone nature and non-selective membrane binding. To address this challenge, we developed a polymer prodrug by conjugating AmB to oxidized chondroitin sulfate (CSox) via a Schiff-base linkage designed to be pH-labile, selected for CS's CD44-targeting capability, intrinsic anti-inflammatory activity, and favorable polyelectrolyte properties. The resulting CSox-AmB conjugate self-assembled into uniform micelles (141.60 ± 4.03 nm, zeta potential -25.47 ± 0.59 mV) with a drug loading of 7.07 ± 0.13%, maintaining AmB predominantly in its monomeric state (A348/A409 = 0.865 < 1). The prodrug exhibited sustained release (∼68% at 24 h) while preserving antifungal activity comparable to free AmB against Candida albicans. Concurrently, it attenuated mammalian cell cytotoxicity by 2.3- to 2.5-fold and markedly attenuated hemolytic activity in vitro (<1% at 25 μg·mL-1). This integrated design-conjugation enabling self-assembly, assembly enabling monomeric stabilization, and controlled release enabling efficacy with markedly reduced toxicity-positions CSox-AmB as a promising prodrug strategy that uncouples the antifungal activity of AmB from its inherent toxicities, warranting further in vivo evaluation toward clinical translation.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-16"},"PeriodicalIF":2.9,"publicationDate":"2026-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149063343","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}

引用次数: 0

Natural biodegradable polymer-based microneedles for controlled drug delivery: a rational design framework and translational perspectives. 天然可生物降解聚合物微针控制药物输送：一个合理的设计框架和翻译的观点。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-24 DOI: 10.1080/10837450.2026.2737199

Khaled E Abuelella, Nermin M Sheta

{"title":"Natural biodegradable polymer-based microneedles for controlled drug delivery: a rational design framework and translational perspectives.","authors":"Khaled E Abuelella, Nermin M Sheta","doi":"10.1080/10837450.2026.2737199","DOIUrl":"10.1080/10837450.2026.2737199","url":null,"abstract":"Microneedle (MN) technology has emerged as a promising minimally invasive platform for transdermal drug delivery, enabling efficient transport of therapeutic agents across the stratum corneum while improving patient compliance. In recent years, natural biodegradable polymers have gained increasing attention in microneedle fabrication due to their biocompatibility, biodegradability, and functional versatility. This review provides a comprehensive overview of recent advances in natural polymer-based microneedle systems, including material selection, fabrication strategies, and mechanisms of controlled drug release. Importantly, beyond conventional descriptive analysis, this work introduces a rational design framework that systematically integrates therapeutic objectives, polymer properties, mechanical performance, and release kinetics to guide the development of optimized microneedle platforms. The review further addresses key translational challenges, including mechanical limitations, manufacturing scalability, stability concerns, and regulatory considerations. In addition, emerging trends such as stimuli-responsive systems, nanocarrier integration, and personalized drug delivery approaches are discussed. Notably, data-driven strategies, including artificial intelligence (AI) and machine learning, are highlighted as promising tools for predicting system performance, optimizing formulation parameters, and accelerating the development of next-generation microneedle-based drug delivery systems. Overall, this work shifts the paradigm from empirical formulation toward a predictive, engineering-driven design strategy, offering valuable insights to advance the clinical translation of smart microneedle technologies.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-22"},"PeriodicalIF":2.9,"publicationDate":"2026-09-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148991107","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}

引用次数: 0

Engineered nanostructured lipid carrier encapsulating thymoquinone and resveratrol to prevent Bisphenol S induced cytotoxicity. 包封百里醌和白藜芦醇的纳米结构脂质载体防止双酚S诱导的细胞毒性。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-21 DOI: 10.1080/10837450.2026.2734054

Garima Sagar, Alok Kumar, Neha Singh, Vikas Srivastava, Somendu Kumar Roy

{"title":"Engineered nanostructured lipid carrier encapsulating thymoquinone and resveratrol to prevent Bisphenol S induced cytotoxicity.","authors":"Garima Sagar, Alok Kumar, Neha Singh, Vikas Srivastava, Somendu Kumar Roy","doi":"10.1080/10837450.2026.2734054","DOIUrl":"10.1080/10837450.2026.2734054","url":null,"abstract":"Nanostructured lipid carriers (NLCs) are diverse colloidal systems that enhance the solubility, stability, and bioavailability of bioactive compounds. Herein, we developed a co-loaded NLC encapsulating thymoquinone (TQ) and resveratrol (RV) to enhance prevention against globally emerging endocrine disruptor bisphenol S (BPS) induced cytotoxicity in NRK-52E cells. The formulation components were rationally optimised, achieving high encapsulation efficiencies for TQ (99.42% ± 0.08) and RV (98.60% ± 0.12), a particle size of 123.66 ± 6.32 nm, and a polydispersity index of 0.37 ± 0.04, indicating stable, homogeneous, quasi-spherical particles as observed in TEM. Interfacial encapsulation and reduced crystallinity observed by FTIR and XRD analyses, respectively, supported the formation of an imperfect core-shell structure. The drug-release profile indicated a diffusion-dominated, matrix-relaxation-assisted transport mechanism. In vitro assays demonstrated a strong cytoprotective effect of TQRV-NLCs at 0.01 μg/mL, comparable to 1 μg/mL free drugs, indicating a significant improvement in therapeutic efficacy. TQRV-NLCs markedly reduced BPS-induced oxidative stress, mitochondrial depolarisation, loss of cell migration, and loss of membrane integrity, while restoring membrane integrity, normalising cell cycle distribution, and preserving nuclear morphology in NRK-52E cells. In summary, this study provides proof of concept that TQRV-NLCs markedly enhance efficacy, confer superior cytoprotection, and offer preventive effects, presenting a promising strategy for renal protection against BPS.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-21"},"PeriodicalIF":2.9,"publicationDate":"2026-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148963602","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}

引用次数: 0

Hydrogen-bonded poly(vinyl alcohol)/tannic acid/quercetin hydrogels for localized controlled drug delivery. 用于局部控制药物递送的氢键聚乙烯醇/单宁酸/槲皮素水凝胶。

IF 2.9 4区医学

Pharmaceutical Development and Technology Pub Date : 2026-09-21 DOI: 10.1080/10837450.2026.2734062

Mina Mohammadi, Mohaddeseh Sadat Mousavi, Shohreh Mohebbi, Mohammad Reza Eskandari, Narges Poursina

{"title":"Hydrogen-bonded poly(vinyl alcohol)/tannic acid/quercetin hydrogels for localized controlled drug delivery.","authors":"Mina Mohammadi, Mohaddeseh Sadat Mousavi, Shohreh Mohebbi, Mohammad Reza Eskandari, Narges Poursina","doi":"10.1080/10837450.2026.2734062","DOIUrl":"10.1080/10837450.2026.2734062","url":null,"abstract":"Localized drug delivery systems provide an effective approach for achieving sustained drug release and prolonged drug retention at the target site while minimizing systemic exposure. In this study, physically crosslinked poly(vinyl alcohol)/tannic acid/quercetin (PVA/TA/Que) (PTQ) hydrogels were developed through hydrogen-bond-mediated self-assembly without chemical crosslinkers. The effect of TA concentration on hydrogel formation, structural properties, thermal stability, swelling, degradation, and release behavior was systematically investigated. Increasing TA concentration accelerated gelation, increased gel content, and produced denser hydrogel networks with lower porosity, reduced water uptake, slower degradation, and improved thermal stability. FT-IR and XRD analysis confirmed hydrogen-bond interactions between PVA and TA and reduced polymer crystallinity. PT50 exhibited the most favorable physicochemical properties and was selected for further evaluation. TA encapsulation efficiency exceeded 93%. In vitro studies demonstrated sustained and pH-responsive TA release, with only 27.39 ± 1.14% released over 312 h at pH 7.4, while Que showed a faster release profile. Hemocompatibility assays revealed hemolysis values below 2%, and hematological, biochemical, and histopathological analysis following subcutaneous implantation in rats showed no detectable systemic toxicity. Overall, the PTQ hydrogels demonstrated favorable physicochemical properties, controlled release behavior, excellent hemocompatibility, and good in vivo biosafety, indicating their potential for localized delivery of bioactive agents.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-15"},"PeriodicalIF":2.9,"publicationDate":"2026-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148963586","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}

引用次数: 0