Erythromycin-loaded polymeric micelles: In situ gel development, in vitro and ex vivo ocular investigations

被引：15

作者：

Sipos, Bence ^{[1
]}

Budai-Szucs, Maria ^{[1
]}

Kokai, David ^{[2
,3
]}

Orosz, Laszlo ^{[2
,3
]}

Burian, Katalin ^{[2
,3
]}

Csorba, Anita ^{[4
]}

Nagy, Zoltan Zsolt ^{[4
]}

Balogh, Gyorgy Tibor ^{[5
,6
]}

Csoka, Ildiko ^{[1
]}

Katona, Gabor ^{[1
]}

机构：

[1] Univ Szeged, Fac Pharm, Inst Pharmaceut Technol & Regulatory Affairs, Eotvos Str 6, H-6720 Szeged, Hungary

[2] Univ Szeged, Albert Szent Gyorgyi Hlth Ctr, Dept Med Microbiol, Semmelweis Str 6, H-6725 Szeged, Hungary

[3] Univ Szeged, Albert Szent Gyorgyi Med Sch, Semmelweis Str 6, H-6725 Szeged, Hungary

[4] Semmelweis Univ, Dept Ophthalmol, Maria Str 39, H-1085 Budapest, Hungary

[5] Univ Szeged, Fac Pharm, Dept Pharmacodynam & Biopharm, Eotvos Str 6, H-6720 Szeged, Hungary

[6] Budapest Univ Technol & Econ, Dept Chem & Environm Proc Engn, Muegyet Quay 3, H-1111 Budapest, Hungary

来源：

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS | 2022年 / 180卷

关键词：

Polymeric micelle; In situ gelling system; Ocular delivery; Nanomedicine; Erythromycin; NONIONIC SURFACTANTS; DRUG-DELIVERY; FORMULATION;

D O I：

10.1016/j.ejpb.2022.09.023

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Our present series of experiments was to create a value-added formulation that has the potential to exert a powerful and long-lasting antibacterial effect for use in ophthalmology. Erythromycin-loaded polymeric micelles were formulated with a micelle size of 87.14 nm in a monodisperse distribution with 86.94 % encapsulation efficiency. To decrease the polymeric micelle-like burst effect of these nanoparticles, the formulation was dispersed in a Carbopol 934P gel base to prolong the drug release and permeation profile of erythromycin. With successful incorporation, a short gelling time with proper sol to gel transition was experienced in the form of transparent gels. The optimized formulation has high mucoadhesion which is a critical factor for prolonging residence time. With the initial burst, the drug release was saturated with more than 75 % of the drug released in simulated tear fluid. Corneal permeability investigations revealed that the gel formulation provides the value-added properties of polymeric micelles, with elevated permeability through into the aqueous humour across the cornea. While retaining its antimicrobial activity, the formulation may be capable to be utilized as an innovative ophthalmic formulation for treating bacterial infections of the eye.

引用

页码：81 / 90

页数：10

共 28 条

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