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Preparation and Evaluation of Topically Applied Azithromycin Based on Sodium Hyaluronate in Treatment of Conjunctivitis

1,2, 1,2, 3, 1,2,* and 1,2,*
1
Department of Pharmaceutics, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China
2
Center for Research Development and Evaluation of Pharmaceutical Excipients and Generic Drugs, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China
3
School of Biomedical Sciences, Faculty of Medicine, the Chinese University of Hong Kong, Hong Kong 999077, China
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2019, 11(4), 183; https://doi.org/10.3390/pharmaceutics11040183
Received: 16 February 2019 / Revised: 25 March 2019 / Accepted: 11 April 2019 / Published: 15 April 2019
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Abstract

Azithromycin (AZI) eye drops containing sodium hyaluronate (SH) were developed to improve the bioavailability of AZI. Interaction between AZI and SH in the AZI-SH formulation was investigated by differential scanning calorimetry, X-ray diffraction, and 1H-nuclear magnetic resonance spectroscopy analyses. Moreover, advantages of using SH as an excipient were investigated by comparing physiological properties and pharmacokinetic behaviors of SH-containing AZI eye drops with that of hydroxypropyl methylcellulose (HPMC)-containing formulation. In addition, safety of the developed AZI-SH eye drops was evaluated by in vitro 3-(4,5-dimethyl-2-Thiazyl)-2, 5-diphenyl-2H-tetrazolium bromide assay (MTT assay) and neutral red uptake assay as well as in vivo eye irritation test and acute toxicity test. The results indicated that AZI formed a complex with SH under a slightly acidic condition. The area under the curve (AUC) of AZI in SH-containing formulation was 1.58-fold higher (P < 0.01) than that in HPMC-containing formulation due to the interaction between the amine group of AZI and the carboxyl group of SH, despite of the higher viscosity of HPMC-containing formulation. Safety evaluation showed that AZI-SH eye drops caused no obvious eye irritation and acute toxicity. In conclusion, the developed SH-containing AZI formulation possessing advantages of longer retention time and higher drug availability was a promising drug formulation for topical ocular therapy. View Full-Text
Keywords: azithromycin; sodium hyaluronate; bioadhesion; eye drops; ocular bioavailability; safety evaluation azithromycin; sodium hyaluronate; bioadhesion; eye drops; ocular bioavailability; safety evaluation
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Chen, Q.; Yin, C.; Ma, J.; Tu, J.; Shen, Y. Preparation and Evaluation of Topically Applied Azithromycin Based on Sodium Hyaluronate in Treatment of Conjunctivitis. Pharmaceutics 2019, 11, 183.

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