Encapsulation of Azithromycin Ion Pair in Liposome for Enhancing Ocular Delivery and Therapeutic Efficacy on Dry Eye
| Autor: | Jingxin Gou, Dongmei You, Xiaoyang Lin, Tianyang Ren, Haibing He, Xiaoguang Tao, Yu Zhang, Xing Tang, Qianying Zhang, Tian Yin, Xiaoyu Liu |
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| Rok vydání: | 2018 |
| Předmět: |
Male
Drug Compounding Pharmaceutical Science Administration Ophthalmic 02 engineering and technology Azithromycin Permeability Cornea Rats Sprague-Dawley 03 medical and health sciences 0302 clinical medicine Differential scanning calorimetry Drug Discovery Zeta potential medicine Animals Humans Fourier transform infrared spectroscopy Hyaluronic Acid Liposome Chemistry Ion pairs 021001 nanoscience & nanotechnology Anti-Bacterial Agents Rats Disease Models Animal Treatment Outcome Liposomes 030221 ophthalmology & optometry Molecular Medicine Nanoparticles Dry Eye Syndromes Particle size Rabbits Ophthalmic Solutions 0210 nano-technology Benzalkonium Compounds Powder diffraction Nuclear chemistry medicine.drug |
| Zdroj: | Molecular pharmaceutics. 15(11) |
| ISSN: | 1543-8392 |
| Popis: | The aim of this work was to design a novel ocular delivery carrier based on liposomes loaded with azithromycin (AZM) for the treatment of dry eye (DE) disease. To improve the drug loading efficiency, an AZM-cholesteryl hemisuccinate (CHEMS) ion pair (ACIP) was first prepared, and the successful formation of the ACIP was characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRD), which demonstrated a stable interaction between CHEMS and AZM. The ACIP-loaded liposome (ACIP-Lip) appeared as spherical particles under TEM, with a uniform particle size of 60 ± 2 nm and zeta potential of -20.3 ± 4.6 mV. The entrapment efficiency (EE) and drug loading (DL) of ACIP-Lip were greatly improved to 95.6 ± 2.0 and 9.2 ± 0.7%, respectively, which was attributed to the enhanced loading capacity of the liposomes through use of the ion pair and addition of MCT. ACIP-Lip also exhibited a high stability during a 3 month storage period at both 4 and 25 °C. In vitro release of AZM from ACIP-Lip was pH-dependent, with a more rapid release at pH 6.0 than at pH 7.4, which is beneficial for ocular therapy. Furthermore, the corneal permeation of AZM was enhanced by ACIP-Lip, demonstrating an apparent permeability coefficient ( P |
| Databáze: | OpenAIRE |
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