Bhattacharyya Sayani, Reddy Priyanka
Krupanidhi College of Pharmacy, Department of Pharmaceutics, Bangalore, India.
Turk J Pharm Sci. 2019 Dec;16(4):425-431. doi: 10.4274/tjps.galenos.2018.82160. Epub 2019 Nov 11.
Azithromycin dihydrate is a macrolide antibiotic used for the treatment of several types of bacterial infections. The drug shows low oral bioavailability due to its low solubility. In the present work solid lipid nanoparticles of azithromycin dihydrate were formulated, keeping in view enhancement of the solubility and rate of dissolution of the drug.
Azithromycin dihydrate loaded stearic acid nanoparticles were formulated by high shear homogenization using three different surfactants, namely Tween 20, poloxamer 188, and poloxamer 407, at a varied lipid surfactant ratio while keeping the quantities of the active ingredient constant. Twelve such formulations were prepared. The nanoparticles obtained were evaluated for drug content, % drug loading, % entrapment efficiency, particle size analysis, zeta potential, surface morphology, Fourier transmission infrared spectroscopy, drug release, and stability.
All the formulations showed good entrapment efficiency and high percentage of release with a particle size suitable for lymphatic absorption. The nanoparticles formulated with poloxamer 188 showed better characteristics compared to the other surfactants.
This study indicates that stearic acid nanoparticles of azithromycin dihydrate prepared by high shear homogenization can be successively used for improvement of dissolution and thereby oral bioavailability of the drug.
二水阿奇霉素是一种用于治疗多种细菌感染的大环内酯类抗生素。由于其低溶解度，该药物口服生物利用度较低。在本研究中，制备了二水阿奇霉素的固体脂质纳米粒，旨在提高药物的溶解度和溶出速率。
采用高剪切均质法，使用三种不同的表面活性剂（吐温20、泊洛沙姆188和泊洛沙姆407），以不同的脂质-表面活性剂比例制备负载二水阿奇霉素的硬脂酸纳米粒，同时保持活性成分的量恒定。共制备了12种这样的制剂。对所得纳米粒进行药物含量、载药量、包封率、粒径分析、zeta电位、表面形态、傅里叶变换红外光谱、药物释放和稳定性评估。
所有制剂均显示出良好的包封率和高释放百分比，且粒径适合淋巴吸收。与其他表面活性剂相比，用泊洛沙姆188制备的纳米粒表现出更好的特性。
本研究表明，通过高剪切均质法制备的二水阿奇霉素硬脂酸纳米粒可成功用于改善药物的溶出度，从而提高其口服生物利用度。
