Preparation and Evaluation of Resveratrol-Loaded Composite Nanoparticles Using a Supercritical Fluid Technology for Enhanced Oral and Skin Delivery

被引：47

作者：

Ha, Eun-Sol ^{[1
]}

Sim, Woo-Yong ^{[1
]}

Lee, Seon-Kwang ^{[1
]}

Jeong, Ji-Su ^{[1
]}

Kim, Jeong-Soo ^{[2
]}

Baek, In-hwan ^{[3
]}

Choi, Du Hyung ^{[4
]}

Park, Heejun ^{[5
]}

Hwang, Sung-Joo ^{[6
,7
]}

Kim, Min-Soo ^{[1
]}

机构：

[1] Pusan Natl Univ, Coll Pharm, 63 Busandaehak Ro, Busan 46241, South Korea

[2] Dong A ST Co Ltd, Yongin 446905, South Korea

[3] Kyungsung Univ, Coll Pharm, 309 Suyeong Ro, Busan 48434, South Korea

[4] Inje Univ, Dept Pharmaceut Engn, Gyeongnam 621749, South Korea

[5] Purdue Univ, Coll Pharm, Dept Ind & Phys Pharm, 575 Stadium Mall Dr, W Lafayette, IN 47907 USA

[6] Yonsei Univ, Coll Pharm, 85 Songdogwahak Ro, Incheon 21983, South Korea

[7] Yonsei Univ, Yonsei Inst Pharmaceut Sci, 85 Songdogwahak Ro, Incheon 21983, South Korea

来源：

ANTIOXIDANTS | 2019年 / 8卷 / 11期

基金：

新加坡国家研究基金会;

关键词：

resveratrol; solubility; nanoparticle; correlation; supercritical fluid; bioavailability; TRANS-RESVERATROL; VIVO EVALUATION; DRUG-DELIVERY; SOLUBLE DRUGS; BIOAVAILABILITY; FORMULATION; MICRONIZATION; PENETRATION; DISSOLUTION; PERMEATION;

D O I：

10.3390/antiox8110554

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We created composite nanoparticles containing hydrophilic additives using a supercritical antisolvent (SAS) process to increase the solubility and dissolution properties of trans-resveratrol for application in oral and skin delivery. Physicochemical properties of trans-resveratrol-loaded composite nanoparticles were characterized. In addition, an in vitro dissolution-permeation study, an in vivo pharmacokinetic study in rats, and an ex vivo skin permeation study in rats were performed. The mean particle size of all the composite nanoparticles produced was less than 300 nm. Compared to micronized trans-resveratrol, the trans-resveratrol/hydroxylpropylmethyl cellulose (HPMC)/poloxamer 407 (1:4:1) nanoparticles with the highest flux (0.792 mu g/min/cm(2)) exhibited rapid absorption and showed significantly higher exposure 4 h after oral administration. Good correlations were observed between in vitro flux and in vivo pharmacokinetic data. The increased solubility and flux of trans-resveratrol generated by the HPMC/surfactant nanoparticles increased the driving force on the gastrointestinal epithelial membrane and rat skin, resulting in enhanced oral and skin delivery of trans-resveratrol. HPMC/surfactant nanoparticles produced by an SAS process are, thus, a promising formulation method for trans-resveratrol for healthcare products (owing to their enhanced absorption via oral administration) and for skin application with cosmetic products.

引用

页数：17

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