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

D. Holmkvist, AlexanderLund University,Lunds universitet,Neurofysiologi,Forskargrupper vid Lunds universitet,Neuronano Research Center (NRC),Centrum för analys och syntes,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Neurophysiology,Lund University Research Groups,Centre for Analysis and Synthesis,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH (author)

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 220nm 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 time compared to what has hitherto been achieved for minocycline and indicate that such particles might provide useful for sustained drug delivery in the CNS.

Friberg, AnnikaLund University,Lunds universitet,Neuronano Research Center (NRC),Forskargrupper vid Lunds universitet,Lund University Research Groups(Swepub:lu)orgk1-af (author)
Nilsson, UlfLund University,Lunds universitet,Centrum för analys och syntes,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Centre for Analysis and Synthesis,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH(Swepub:lu)ok2-uni (author)
Schouenborg, JensLund University,Lunds universitet,Neurofysiologi,Forskargrupper vid Lunds universitet,Neuronano Research Center (NRC),Neurophysiology,Lund University Research Groups(Swepub:lu)mphy-jsc (author)
NeurofysiologiForskargrupper vid Lunds universitet (creator_code:org_t)

In:International Journal of Pharmaceutics: Elsevier BV499:1-2, s. 351-3571873-34760378-5173

By the author/editor: D. Holmkvist, Al ...; Friberg, Annika; Nilsson, Ulf; Schouenborg, Jen ...

About the subject

MEDICAL AND HEALTH SCIENCES: MEDICAL AND HEAL ...; and Basic Medicine; and Pharmaceutical S ...

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