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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

Yu, Yongjun, Ngo, Hai V, Jin, Gang, Tran, Ha Lien Phuong, Tran, Thao TD, Nguyen, Van Hong, Park, Chulhun and Lee, Beom-Jin 2021, Double-controlled release of poorly water-soluble paliperidone palmitate from self-assembled albumin-oleic acid nanoparticles in plga in situ forming implant, International journal of nanomedicine, vol. 16, pp. 2819-2831, doi: 10.2147/IJN.S302514.

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Title Double-controlled release of poorly water-soluble paliperidone palmitate from self-assembled albumin-oleic acid nanoparticles in plga in situ forming implant
Author(s) Yu, Yongjun
Ngo, Hai V
Jin, Gang
Tran, Ha Lien PhuongORCID iD for Tran, Ha Lien Phuong orcid.org/0000-0001-8463-7516
Tran, Thao TD
Nguyen, Van Hong
Park, Chulhun
Lee, Beom-Jin
Journal name International journal of nanomedicine
Volume number 16
Start page 2819
End page 2831
Total pages 13
Publisher Dove Medical Press
Place of publication Macclesfield, Eng.
Publication date 2021
ISSN 1176-9114
1178-2013
Keyword(s) albumin-oleic acid conjugate
controlled release
in situ forming implant
self-assembled nanonization
solvent exchange
solvent type
Summary 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.
Language eng
DOI 10.2147/IJN.S302514
Indigenous content off
Field of Research 0601 Biochemistry and Cell Biology
1007 Nanotechnology
1115 Pharmacology and Pharmaceutical Sciences
HERDC Research category C1 Refereed article in a scholarly journal
Free to Read? Yes
Persistent URL http://hdl.handle.net/10536/DRO/DU:30150632

Document type: Journal Article
Collections: Faculty of Health
School of Medicine
Open Access Collection
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Every reasonable effort has been made to ensure that permission has been obtained for items included in DRO. If you believe that your rights have been infringed by this repository, please contact drosupport@deakin.edu.au.