期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 516, 期 1-2, 页码 196-203出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2016.10.072
关键词
Vitamin D3; TyroSpheres; Nanoparticles; Skin permeation; Photostability
资金
- National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS - NIH) [5R01AR056079]
- Center for Dermal Research CDR
- NJ Center for Biomaterials, Rutgers-The State University of New Jersey, Piscataway NJ
This study investigates the potential application of polymeric nanospheres (known as TyroSpheres) as a formulation carrier for topical delivery of cholecalciferol (i.e., Vitamin D3, VD3) with the goal to improve the skin delivery and stability of VD3. High drug loading and binding efficiencies were obtained for VD3 when loaded in TyroSpheres. VD3 was released from TyroSpheres in a sustained manner and was delivered across the stratum corneum, which occurred independent of the initial drug loading. An ex vivo skin distribution study showed that TyroSphere formulations delivered 3-10 mu g of active into the epidermis which was significantly higher than that delivered from Transcutol (R) (the control vehicle). In addition, an in vitro cytotoxicity assay using keratinocytes confirmed that VD3 encapsulation in the nanoparticles did not alter the drug activity. Photodegradation of VD3 followed zero-order kinetics. TyroSpheres were able to protect the active against hydrolysis and photodegradation, significantly enhancing the stability of VD3 in the topical formulation. (C) 2016 Elsevier B.V. All rights reserved.
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