Development and Evaluation of Astaxanthin as Nanostructure Lipid Carriers in Topical Delivery
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Research Article Theme: Formulation and Delivery of Natural Products Guest Editors: Harsh Chauhan, Abhijit Date and Sonali Dhindwal
Development and Evaluation of Astaxanthin as Nanostructure Lipid Carriers in Topical Delivery Qiang Geng,1 Yuming Zhao,1 Lu Wang,1 Lulu Xu,1 Xiong Chen,1 and Jing Han1,2,3
Received 22 April 2020; accepted 16 September 2020 Abstract. The study is designed to formulate, optimize, and evaluate astaxanthin (ASTA)loaded nanostructured lipid carrier (NLC) with an aim to improve its stability, water solubility, skin permeability and retention and reduce drug-related side effects. ASTA was extracted from Haematococcus pluvialis. ASTA-NLC was formulated by the technique of melt emulsification—ultrasonic and optimized taking solid:liquid lipid ratio, total lipid:drug ratio, drug concentration, emulsifier types, and amounts as independent variables with particle sizes (PS) and entrapment efficiency (EE) as dependent variables. The optimized formulation (N21) exhibited spherical surfaced stable nanoparticles of 67.4 ± 2.1 nm size and 94.3 ± 0.5% EE. Formulation N21 was then evaluated for its physiological properties, physicochemical properties, drug content, in vitro release and skin penetration, and retention analysis. The ASTA-NLC was found to be nonirritating, homogenous, and with excellent stability and water solubility. In vitro release studies showed the cumulative release rate of NLC was 83.0 ± 3.4% at 48 h. The skin penetration and retention studies indicated that cumulative permeability was 174.10 ± 4.38 μg/cm2 and the retention was 8.00 ± 1.62 μg/cm2 within 24 h. It can be concluded that NLC serves as a promising carrier for site specific targeting with better stability and skin penetration. KEY WORDS: astaxanthin; nanostructured lipid carriers; development; evaluation; transdermal absorption.
INTRODUCTION The raising living standards boost the development of cosmeceuticals, especially with ingredients that reduce the oxidative stress and cellular damage of skin. Astaxanthin (ASTA, Fig. 1) is a lipid-soluble keto-carotenoid with superior antioxidant activity (1) and related anti-inflammatory/antiapoptotic effects both in vitro and in vivo (2). Other biological activities include anticancer (3), reduction of plasma cholesterol (4), relief of eyestrain (5), etc. Natural ASTA has been approved for the use as coloring agent for animal and aquatic feeds by different agencies such as the Guest Editors: Harsh Chauhan, Abhijit Date and Sonali Dhindwal Supplementary Information The online version of this article (https:// doi.org/10.1208/s12249-020-01822-w) contains supplementary material, which is available to authorized users. 1
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Benxi, 117004, China. 2 School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, NO.26, Huatuo Street, Xihu District, Benxi City, 117004, Liaoning Province, China. 3 To whom correspondence should be addressed. (e–mail: [email protected])
Food and Drug Administration (FDA) and Europea
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