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Open AccessArticle

Effect of Polymer Permeability and Solvent Removal Rate on In Situ Forming Implants: Drug Burst Release and Microstructure

1
Department of Pharmaceutics, School of Pharmacy, China Medical University, Liaoning 110122, China
2
Key Laboratory of Reproductive Health, Liaoning Research Institute of Family Planning, Liaoning 110031, China
3
Shenyang Institute for Drug Control, Liaoning 110084, China
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(10), 520; https://doi.org/10.3390/pharmaceutics11100520
Received: 2 September 2019 / Revised: 26 September 2019 / Accepted: 8 October 2019 / Published: 10 October 2019
To explore the mechanism of drug release and depot formation of in situ forming implants (ISFIs), osthole-loaded ISFIs were prepared by dissolving polylactide, poly(lactide-co-glycolide), polycaprolactone, or poly(trimethylene carbonate) in different organic solvents, including N-methyl-2-pyrrolidone (NMP), dimethyl sulfoxide (DMSO), and triacetin (TA). Drug release, polymer degradation, solvent removal rate and depot microstructure were examined. The burst release effect could be reduced by using solvents exhibit slow forming phase inversion and less permeable polymers. Both the drug burst release and polymer depot microstructure were closely related to the removal rate of organic solvent. Polymers with higher permeability often displayed faster drug and solvent diffusion rates. Due to high polymer-solvent affinity, some of the organic solvent remained in the depot even after the implant was completely formed. The residual of organic solvent could be predicted by solubility parameters. The ISFI showed a lower initial release in vivo than that in vitro. In summary, the effects of different polymers and solvents on drug release and depot formation in ISFI systems were extensively investigated and discussed in this article. The two main factors, polymer permeability and solvent removal rate, were involved in different stages of drug release and depot formation in ISFI systems. View Full-Text
Keywords: in situ forming implant; burst release; permeability; solvent exchange; degradation in situ forming implant; burst release; permeability; solvent exchange; degradation
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MDPI and ACS Style

Zhang, X.; Yang, L.; Zhang, C.; Liu, D.; Meng, S.; Zhang, W.; Meng, S. Effect of Polymer Permeability and Solvent Removal Rate on In Situ Forming Implants: Drug Burst Release and Microstructure. Pharmaceutics 2019, 11, 520. https://doi.org/10.3390/pharmaceutics11100520

AMA Style

Zhang X, Yang L, Zhang C, Liu D, Meng S, Zhang W, Meng S. Effect of Polymer Permeability and Solvent Removal Rate on In Situ Forming Implants: Drug Burst Release and Microstructure. Pharmaceutics. 2019; 11(10):520. https://doi.org/10.3390/pharmaceutics11100520

Chicago/Turabian Style

Zhang, Xiaowei; Yang, Liqun; Zhang, Chong; Liu, Danhua; Meng, Shu; Zhang, Wei; Meng, Shengnan. 2019. "Effect of Polymer Permeability and Solvent Removal Rate on In Situ Forming Implants: Drug Burst Release and Microstructure" Pharmaceutics 11, no. 10: 520. https://doi.org/10.3390/pharmaceutics11100520

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