Development of Gentamicin Bilosomes Laden In Situ Gel for Topical Ocular Delivery: Optimization, In Vitro Characterization, Toxicity, and Anti-microbial Evaluation.

IF 3.1 Q2 PHARMACOLOGY & PHARMACY Advanced pharmaceutical bulletin Pub Date : 2024-10-01 Epub Date: 2024-07-31 DOI:10.34172/apb.2024.057
Ameeduzzafar Zafar, Omar Awad Alsaidan, Malik Suliman Mohamed, Mohd Yasir, Mohammad Khalid
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Abstract

Purpose: The eye drops are the prominent preparation used to treat surface eye disease (bacterial conjunctivitis). However, they have some limitations i.e., short corneal residence, resulting in low ocular bioavailability and necessitating frequent dose administration. The present study developed gentamicin (GE) bilosomes (BM)- laden in situ gel to improve therapeutic activity. The in situ gel system is initially in sol form before administration and converted into gel form in physiological eye conditions.

Methods: The GE-BM was developed using the thin film hydration technique and optimized by D-optimal design. GE-BM was characterized for vesicle size, entrapment efficiency, zeta potential, morphology, and Fourier transform electron microscope (FTIR). The optimized GE-BM (GE-BMopt) was incorporated into an in situ gel and assessed for physicochemical characteristics. GE-BMopt in situ gel was evaluated for in vitro release, ex vivo permeation, toxicity, and antimicrobial study.

Results: GE-BMopt has a vesicle size of 185.1±4.8nm, PDI of 0.254, zeta potential of 27.6 mV, entrapment efficiency of 81.86±1.29 %, and spherical morphology. The FTIR study presented no chemical interactions between GE and excipients. GE-BMopt in situ gel (GE-BMoptIG4) showed excellent viscosity, gelling strength, and ex-vivo bio-adhesion. GE-BMopt-IG4 showed significant high and sustained release of GE (78.08±4.73% in 12h). GE-BMopt-IG4 displayed 3.27-fold higher ex-vivo goat corneal permeation than a pure GE solution. GE-BMopt-IG4 showed good corneal tolerance without any damage or irritation. GE-BMopt-IG4 showed significantly (P<0.05) higher anti-bacterial activity (ZOI) against Staphylococcus aureus and Escherichia coli than pure GE solution.

Conclusion: The study determined that the BM in situ gel system can serve as a substitute carrier for GE to enhance its therapeutic effectiveness, and further preclinical studies are required.

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用于局部眼部给药的庆大霉素双体载体原位凝胶的开发:优化、体外表征、毒性和抗微生物评估。
目的:滴眼液是治疗表面眼病(细菌性结膜炎)的主要制剂。然而,眼药水也有一些局限性,如在角膜停留时间短,导致眼部生物利用度低,需要频繁给药。本研究开发了含有庆大霉素(GE)双载体(BM)的原位凝胶,以提高治疗活性。该原位凝胶系统在给药前最初为溶胶状,在眼部生理条件下转化为凝胶状:方法:利用薄膜水合技术开发了 GE-BM,并通过 D-优化设计进行了优化。对 GE-BM 的囊泡大小、包埋效率、zeta 电位、形态和傅立叶变换电子显微镜(FTIR)进行了表征。将优化后的 GE-BM (GE-BMopt)加入原位凝胶中,并对其理化特性进行评估。对 GE-BMopt 原位凝胶进行了体外释放、体内渗透、毒性和抗菌研究评估:结果:GE-BMopt 的囊泡大小为 185.1±4.8nm,PDI 为 0.254,zeta 电位为 27.6 mV,夹带效率为 81.86±1.29%,形态为球形。傅立叶变换红外光谱研究表明,GE 与辅料之间没有化学作用。GE-BMopt原位凝胶(GE-BMoptIG4)显示出优异的粘度、胶凝强度和体内外生物粘附性。GE-BMopt-IG4 显示出显著的高持续释放性(12 小时内释放 78.08±4.73%)。与纯 GE 溶液相比,GE-BMopt-IG4 的体外山羊角膜渗透率高出 3.27 倍。GE-BMopt-IG4 显示出良好的角膜耐受性,没有任何损伤或刺激。与纯 GE 溶液相比,GE-BMopt-IG4 的金黄色葡萄球菌和大肠杆菌数量明显减少:该研究确定了 BM 原位凝胶系统可作为 GE 的替代载体,以提高其治疗效果,但还需要进一步的临床前研究。
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来源期刊
Advanced pharmaceutical bulletin
Advanced pharmaceutical bulletin PHARMACOLOGY & PHARMACY-
CiteScore
6.80
自引率
2.80%
发文量
51
审稿时长
12 weeks
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