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Double-controlled release of poorly water-soluble paliperidone palmitate from self-assembled albumin-oleic acid nanoparticles in plga in situ forming implant

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Version 2 2024-06-06, 02:53
Version 1 2021-05-06, 09:03
journal contribution
posted on 2024-06-06, 02:53 authored by Y Yu, HV Ngo, G Jin, PHL Tran, TTD Tran, VH Nguyen, C Park, BJ Lee
Purpose: To investigate the effects of solvents on the formation of self-assembled nanoni-zation of albumin-oleic acid conjugates (AOCs) using a solvent exchange mechanism for the construction of in situ forming implants (ISFI). Methods: A poorly water-soluble drug, paliperidone palmitate (PPP), was chosen as the model drug. AOC was synthesized with the 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC) reaction. Dichloromethane, tetrahydrofuran, ethanol, N-methyl-2-pyrrolidone, dimethyl sulfoxide, and deionized water were selected to investigate the formation of self-assembled AOC nanoparticles (AONs). The volume ratios of organic solvents against water could determine the miscibility, injectability, and in situ nanonizing capability without aggregation. Results: As the polarity of the organic solvents increased, the AONs exhibited a spherical shape, and the larger the volume of the solvent, the smaller the size of the AONs. To use AOC in ISFI for controlled release of PPP, poly(d,l-lactide-co-glycolide) (PLGA) was combined with the AOC in 2 mL of N-methyl-2-pyrrolidone and water solution (1.8/0.2 ratio). The release rates of all formulations exhibited similar curve patterns overall but were more controlled in decreasing order as follows: AOC, PLGA, and AOC/PLGA for 14 days. Conclusion: A combined formulation of AOC and PLGA was found to effectively control the initial burst release of the drug.

History

Journal

International journal of nanomedicine

Volume

16

Pagination

2819-2831

Location

Macclesfield, Eng.

ISSN

1176-9114

eISSN

1178-2013

Language

eng

Publication classification

C1 Refereed article in a scholarly journal

Publisher

Dove Medical Press