期刊
POLYMERS
卷 13, 期 23, 页码 -出版社
MDPI
DOI: 10.3390/polym13234207
关键词
drug delivery; polymer-lipid hybrid nanoparticles; curcumin; demethoxycurcumin; bisdemethoxycurcumin; Pluronic F-127
资金
- University of Costa Rica [115-B8-150, 115-C1-501]
- National Laboratory of Nanotechnology (LANOTEC)
The PLHNs are developed as drug delivery systems with improved bioactivity by successfully encapsulating different curcuminoids and molecules using a simple method, showing increased release and enhanced antioxidant activity compared to free compounds.
Polymeric lipid hybrid nanoparticles (PLHNs) are the new generation of drug delivery systems that has emerged as a combination of a polymeric core and lipid shell. We designed and optimized a simple method for the preparation of Pluronic F-127-based PLHNs able to load separately demethoxycurcumin (DMC) and bisdemethoycurcumin (BDM). CUR was used as a model compound due to its greater availability from turmeric and its structure similarity with DMC and BDM. The developed method produced DMC and BDM-loaded PLHNs with a size average of 75.55 +/- 0.51 and 15.13 +/- 0.014 nm for DMC and BDM, respectively. An FT-IR analysis confirmed the encapsulation and TEM images showed their spherical shape. Both formulations achieved an encapsulation efficiency >= 92% and an exhibited significantly increased release from the PLHN compared with free compounds in water. The antioxidant activity was enhanced as well, in agreement with the improvement in water dissolution; obtaining IC50 values of 12.74 +/- 0.09 and 16.03 +/- 0.55 for DMC and BDM-loaded PLHNs, respectively, while free curcuminoids exhibited considerably lower antioxidant values in an aqueous solution. Hence, the optimized PHLN synthesis method using CUR as a model and then successfully applied to obtain DMC and BDM-loaded PLHNs can be extended to curcuminoids and molecules with a similar backbone structure to improve their bioactivities.
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