Yan Liu1, Xia Lin, Xing Tang. 1. Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, 110016, PR China.
Abstract
OBJECTIVE: To obtain stable positively charged Azithromycin (AZI) emulsions with a mean droplet size of 120 nm for the treatment of eye diseases. METHODS: The emulsions were obtained by using a suitable homogenization process. The physical stability was monitored by measuring the particle size, zeta potential, and visible appearance. The drug entrapment efficiency was measured by both ultracentrifugation and ultrafiltration methods. Compared with a phosphate solution of AZI, the stability profiles of AZI in lipid emulsions at various pH values were monitored by high-performance liquid chromatography. A pharmacokinetic study was performed to determine the drug levels in rabbit tear fluid using Ultra-performance liquid Chromatography-mass spectrometry. RESULTS: Almost all the AZI in the lipid emulsion was distributed in the oil phase and small unilamellar liposomes without contact with water, thereby avoiding hydrolysis. The elimination of the AZI lipid emulsions in tear fluid was consistent with the basic linear pharmacokinetic characteristics. The AUC(0-t) of the AZI lipid emulsion (1%, w/v) and aqueous solution drops (1%, w/v) was 1873.58 +/- 156.87 and 1082.46 +/- 179.06 mugh/ml respectively. CONCLUSIONS: This study clearly describes a new formulation of AZI lipid emulsion for ocular administration, and lipid emulsions are promising vehicles for ophthalmic drug delivery.
OBJECTIVE: To obtain stable positively charged Azithromycin (AZI) emulsions with a mean droplet size of 120 nm for the treatment of eye diseases. METHODS: The emulsions were obtained by using a suitable homogenization process. The physical stability was monitored by measuring the particle size, zeta potential, and visible appearance. The drug entrapment efficiency was measured by both ultracentrifugation and ultrafiltration methods. Compared with a phosphate solution of AZI, the stability profiles of AZI in lipid emulsions at various pH values were monitored by high-performance liquid chromatography. A pharmacokinetic study was performed to determine the drug levels in rabbit tear fluid using Ultra-performance liquid Chromatography-mass spectrometry. RESULTS: Almost all the AZI in the lipid emulsion was distributed in the oil phase and small unilamellar liposomes without contact with water, thereby avoiding hydrolysis. The elimination of the AZI lipid emulsions in tear fluid was consistent with the basic linear pharmacokinetic characteristics. The AUC(0-t) of the AZI lipid emulsion (1%, w/v) and aqueous solution drops (1%, w/v) was 1873.58 +/- 156.87 and 1082.46 +/- 179.06 mugh/ml respectively. CONCLUSIONS: This study clearly describes a new formulation of AZI lipid emulsion for ocular administration, and lipid emulsions are promising vehicles for ophthalmic drug delivery.
Authors: Eliana B Souto; João Dias-Ferreira; Ana López-Machado; Miren Ettcheto; Amanda Cano; Antonio Camins Espuny; Marta Espina; Maria Luisa Garcia; Elena Sánchez-López Journal: Pharmaceutics Date: 2019-09-06 Impact factor: 6.321
Authors: Jose Navarro-Partida; Carlos Rodrigo Castro-Castaneda; Francisco J Santa Cruz-Pavlovich; Luis Abraham Aceves-Franco; Tomer Ori Guy; Arturo Santos Journal: Pharmaceutics Date: 2021-05-09 Impact factor: 6.321