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盐酸洛美沙星眼用传递载体——前体脂质体的设计与评价

Design and evaluation of proniosomes as a carrier for ocular delivery of lomefloxacin HCl.

作者信息

Khalil Rawia M, Abdelbary Ghada A, Basha Mona, Awad Ghada E A, El-Hashemy Hadeer A

机构信息

a Department of Pharmaceutical Technology , National Research Centre , Cairo , Egypt.

b Department of Pharmaceutics , Faculty of Pharmacy, Cairo University , Cairo , Egypt , and.

出版信息

J Liposome Res. 2017 Jun;27(2):118-129. doi: 10.3109/08982104.2016.1167737. Epub 2016 May 12.

DOI:10.3109/08982104.2016.1167737
PMID:27079800
Abstract

The current investigation aims to develop and evaluate novel ocular proniosomal gels of lomefloxacin HCl (LXN); in order to improve its ocular bioavailability for the management of bacterial conjunctivitis. Proniosomes were prepared using different types of nonionic surfactants solely and as mixtures with Span 60. The formed gels were characterized for entrapment efficiency, vesicle size, and in vitro drug release. Only Span 60 was able to form stable LXN-proniosomal gel when used individually while the other surfactants formed gels only in combination with Span 60 at different ratios. The optimum proniosomal gel; P-LXN 7 (Span 60:Tween 60, 9:1) appeared as spherical shaped vesicles having high entrapment efficiency (>80%), appropriate vesicle size (187 nm) as well as controlled drug release over 12 h. Differential scanning calorimetry confirmed the amorphous nature of LXN within the vesicles. Stability study did not show any significant changes in entrapment efficiency or vesicle size after storage for 3 months at 4 °C. P-LXN 7 was found to be safe and suitable for ocular delivery as proven by the irritancy test. The antibacterial activity of P-LXN 7 evaluated using the susceptibility test and topical therapy of induced ocular conjunctivitis confirmed the enhanced antibacterial therapeutic efficacy of the LXN-proniosomal gel compared to the commercially available LXN eye drops.

摘要

当前的研究旨在开发和评估新型盐酸洛美沙星(LXN)眼部前体脂质体凝胶;以提高其眼部生物利用度,用于治疗细菌性结膜炎。单独使用不同类型的非离子表面活性剂以及与司盘60混合制备前体脂质体。对形成的凝胶进行包封率、囊泡大小和体外药物释放的表征。单独使用时,只有司盘60能够形成稳定的LXN前体脂质体凝胶,而其他表面活性剂仅在与司盘60以不同比例组合时才能形成凝胶。最佳的前体脂质体凝胶;P-LXN 7(司盘60:吐温60,9:1)呈现为球形囊泡,具有高包封率(>80%)、合适的囊泡大小(187nm)以及在12小时内的可控药物释放。差示扫描量热法证实了囊泡内LXN的无定形性质。稳定性研究表明,在4℃储存3个月后,包封率或囊泡大小没有任何显著变化。刺激性试验证明,P-LXN 7安全且适合眼部给药。通过药敏试验和诱导性眼部结膜炎的局部治疗评估的P-LXN 7的抗菌活性证实,与市售的LXN眼药水相比,LXN前体脂质体凝胶的抗菌治疗效果增强。

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