期刊
JOURNAL OF MATERIALS SCIENCE & TECHNOLOGY
卷 63, 期 -, 页码 133-144出版社
JOURNAL MATER SCI TECHNOL
DOI: 10.1016/j.jmst.2020.04.020
关键词
Triptorelin acetate; Peptide delivery; Poly (D, L-lactic-co-glycolic) acid; Microspheres; Long-acting injectable
资金
- Natural Science Foundation of Liaoning province of China-Guidance Plan [2019-ZD-0448]
- Liaoning Province Pan Deng Xue Zhe Grant
The present study successfully formulated TA-PLGA-MS using DESE technique and investigated the effects of various material attributes and process parameters on the quality attributes. An optimal formulation (F-2) with excellent EE and particle size was obtained, and different incubation temperatures impacted the morphology and release behavior of the microspheres.
The present study aimed to formulate triptorelin acetate (TA) into poly (D, L-lactic-co-glycolic) acid (PLGA) based injectable sustained-release microspheres (TA-PLGA-MS) by usingdouble emulsion solvent extraction/evaporation (DESE) technique and investigate the effects of various material attributes and process parameters on the quality attributes such as size, shape, surface morphology, encapsulation efficiency (EE) and in vitro release behavior of these microspheres. Variable compositions of the outer water phase, type of the organic solvents, volume ratios of inner water phase to oil phase, PLGA concentrations, and the powers for emulsification in the preparation of the microspheres showed an influence on their quality attributes. An optimal formulation (F-2) obtained from this univariate approach possess an excellent EE value of 63.5% +/- 3.4% and an average volumetric particle size of 35.3 +/- 1.8 pin. This formulation was further accomplished with different solidification rates assisted by variable incubation temperatures, which exhibited an impact on the shape/surface and inner morphology of the microspheres. The resultant microspheres also displayed different in vitro release patterns. The matrices processed with a high incubation temperature conferred the fastest and the most complete drug release profile over the period of 63 days. Thus, the solidification rate could be identified as one of the critical process parameters that affected the quality of the PLGA based injectable microspheres specifically designed for the prolonged delivery of TA. (C) 2020 Published by Elsevier Ltd on behalf of The editorial office of Journal of Materials Science & Technology.
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