Hydrophobic ion pairing of a minocycline/Ca(2+)/AOT complex for preparation of drug-loaded PLGA nanoparticles with improved sustained release

International Journal of Pharmaceutics
Alexander Dontsios HolmkvistJens Schouenborg

Abstract

Polymeric nanoparticles is an established and efficient means to achieve controlled release of drugs. Incorporation of minocycline, an antibiotic with anti-inflammatory and neuroprotective properties, into biodegradable nanoparticles may therefore provide an efficient means to combat foreign body reactions to implanted electrodes in the brain. However, minocycline is commonly associated with poor encapsulation efficiencies and/or fast release rates due to its high solubility in water. Moreover, minocycline is unstable under conditions of low and high pH, heat and exposure to light, which exacerbate the challenges of encapsulation. In this work drug loaded PLGA nanoparticles were prepared by a modified emulsification-solvent-diffusion technique and characterized for size, drug encapsulation and in vitro drug release. A novel hydrophobic ion pair complex of minocycline, Ca(2+) ions and the anionic surfactant AOT was developed to protect minocycline from degradation and prolong its release. The optimized formulation resulted in particle sizes around 220 nm with an entrapment efficiency of 43% and showed drug release over 30 days in artificial cerebrospinal fluid. The present results constitute a substantial increase in release tim...Continue Reading

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Citations

Dec 8, 2016·Journal of Neurochemistry·Marta Machado-PereiraRaquel Ferreira
Feb 6, 2020·AAPS PharmSciTech·Nermin E ElerakyGiovanni M Pauletti
Sep 21, 2019·Future Medicinal Chemistry·Ming-Hsien LinJia-You Fang
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Dec 30, 2020·Journal of Pharmaceutical Sciences·Linfeng WuLiang Hong
Oct 1, 2019·Nanoscale Advances·Kurt D Ristroph, Robert K Prud'homme
Mar 9, 2021·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Bingxue Dong, Kunn Hadinoto
Jun 8, 2021·ACS Omega·Noa Ben DavidBoaz Mizrahi

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