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J Pharm Sci. 2015 Oct;104(10):3510-23. doi: 10.1002/jps.24547. Epub 2015 Jun 24.

Development and In Vitro Evaluation of Vitamin E-Enriched Nanoemulsion Vehicles Loaded with Genistein for Chemoprevention Against UVB-Induced Skin Damage.

Author information

1
Department of Pharmaceutical Sciences, College of Pharmacy-Glendale, Midwestern University, Glendale, Arizona, 85308.
2
Department of Biochemistry, Midwestern University, Glendale, Arizona, 85308.
3
Midwestern University, College of Pharmacy-Glendale, Glendale, Arizona, 85308.
4
Arizona College of Osteopathic Medicine, Midwestern University, Glendale, Arizona, 85308.

Abstract

There is a great need for effective protection against cutaneous pathologies arising from chronic exposure to harmful solar UVB radiations. A promising pharmaceutical strategy to improve the efficacy of chemotherapeutic/preventative natural compounds (e.g., soy isoflavone Genistein, Gen) is to enhance their dermal delivery using nanoemulsion (NE) formulations. This report investigates the development of nanoemulsified tocotrienol(T3)-rich fraction of red palm oil (Tocomin®), to yield an optimal NE delivery system for dermal photoprotection (z-average size <150 nm, ζ-potential ≈ -30 mV, polydispersity index < 0.25). Physicochemical characterization and photostability studies indicate NE formulations utilizing surfactant mixture (Smix) of Solutol® HS-15 (SHS15) blended with vitamin E TPGS (TPGS) as cosurfactant was significantly superior to formulations that utilized Lutrol® F68 (LF68) as the cosurfactant. A ratio of 60:40 of SHS15-TPGS-NE was further identified as lead Tocomin® NE topical platform using in vitro pharmaceutical skin reactivity studies that assess cutaneous irritancy and cytotoxicity. Prototype Tocomin® NE loaded with the antiphotocarcinogenic molecule Gen (Gen-Tocomin® NE) showed slow-release profile in both liquid and cream forms. Gen-Tocomin® NE also showed excellent biocompatibility, and provided substantial UVB protection to cultured subcutaneous L929 fibroblasts, indicating the great potential of our Tocomin® NE warranting further prototype development as topical pharmaceutical platform for skin photoprotection applications.

KEYWORDS:

biocompatibility; cancer chemoprevention; controlled release; in vitro models; nanoemulsion; photoprotection; physicochemical properties; self-emulsifying; skin reactivity; tocotrienol

PMID:
26108889
DOI:
10.1002/jps.24547
[Indexed for MEDLINE]

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