ZHONG Songyang,ZHENG Hongliang,MAO Kaili, et al. Preparation and characterization of a novel curcumin-nanomicelles gel[J]. JOURNAL OF WEZHOU MEDICAL UNIVERSITY, 2019, 49(3): 184-188.
Abstract:Objective: To prepare the curcumin-loaded nanomicelles with a novel polymer, RRR-a-tocopheryl succinate-grafted-ε-polylysine conjugate (VES-g-ε-PLL), and to characterize it to use silk fibroin as a hydrogel-based matrix to further facilitate topical delivery of curcumin in exploration of a promising potential of this drug delivery system in the treatment of psoriasis. Methods: VES-g-PLL nanomicelles encapsulated with curcumin were prepared by injection method, and the micromorphology, particle size, Zeta potential, encapsulation efficiency, drug loading, and release rate were evaluated. CUR-NMs-gel was then prepared by mixing the CUR-NMs with the SF solution followed by a sonication-induced gelation method. The microscopic morphology, in vitro drug release and skin permeability of CUR-NMs-gel were determined by scanning electron microscopy, HPLC and confocal laser scanning microscopy. Results: The CUR-NMs was granulate-like particles with uniform dispersion. The nanomicelles exhibited an ultra-small hydrodynamic diameter (31.14±7.86) nm and a positive Zeta potential (16.70±1.45) mV. Moreover, curcumin could effectively be encapsulated in the polymeric nanoparticles with encapsulating efficiency of 82.21%±4.32%. The CUR-NMs-gel displayed a 3D network with flocculate of CUR-NMs adhering to its surface. The CUR release curves from the CUR-NMs-gel exhibited an obvious sustained release of DTX in physiological media with no evidence of burst effect, and only 30% of CUR was released from the CUR-NMs-gel at 72 h in pH 7.4 PBS, while 49% of CUR was released from the CUR-NMs. Vivo studies on skin penetration showed that the application of CUR-NMs-gel can significantly increase the transdermal permeability of the drug compared with the curcumin solution gel. Conclusion: The permeable nanomicelles-gel system could realize the sustained release and transdermal absorption of the soluble drug curcumin, which suggested a promising potential of this drug delivery system to treat such inflammatory skin disorders as psoriasis.
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