Skip to main content
Journal cover image

Encapsulation and controlled release of retinol from silicone particles for topical delivery.

Publication ,  Journal Article
Shields, CW; White, JP; Osta, EG; Patel, J; Rajkumar, S; Kirby, N; Therrien, J-P; Zauscher, S
Published in: Journal of controlled release : official journal of the Controlled Release Society
May 2018

Retinol, a derivative of vitamin A, is a ubiquitous compound used to treat acne, reduce wrinkles and protect against conditions like psoriasis and ichthyosis. While retinol is used as the primary active ingredient (AI) in many skin care formulations, its efficacy is often limited by an extreme sensitivity to degrade and toxicity at high concentrations. While microencapsulation is an appealing method to help overcome these issues, few microencapsulation strategies have made a major translational impact due to challenges with complexity, cost, limited protection of the AI and poor control of the release of the AI. We have developed a class of silicone particles that addresses these challenges for the encapsulation, protection and controlled release of retinol and other hydrophobic compounds. The particles are prepared by the sol-gel polymerization of silane monomers, which enables their rapid and facile synthesis at scale while maintaining a narrow size distribution (i.e., CV < 20%). We show that our particles can: (i) encapsulate retinol with high efficiency (>85%), (ii) protect retinol from degradation (yielding a half-life 9× greater than unencapsulated retinol) and (iii) slowly release retinol over several hours (at rates from 0.14 to 0.67 μg cm-2 s-1/2). To demonstrate that the controlled release of retinol from the particles can reduce irritation, we performed a double blind study on human subjects and found that formulations containing our particles were 12-23% less irritating than identical formulations containing Microsponge® particles (an industry standard by Amcol, Inc.). To show that the silicone particles can elicit a favorable biological response, similar to the Microsponge® particles, we applied both formulations to reconstructed human epidermal tissues and found an upregulation of keratin 19 (K19) and a downregulation of K10, indicating that the reduced irritation observed in the human study was not caused by reduced activity. We also found a decrease in the production of interleukin-1α (IL-1α) compared to formulations containing the Microsponge particles, suggesting lower irritation levels and supporting the findings from the human study. Finally, we show that the silicone particles can encapsulate other AIs, including betamethasone, N, N-diethyl-meta-toluamide (DEET), homosalate and ingenol mebutate, establishing these particles as a true platform technology.

Duke Scholars

Altmetric Attention Stats
Dimensions Citation Stats

Published In

Journal of controlled release : official journal of the Controlled Release Society

DOI

EISSN

1873-4995

ISSN

0168-3659

Publication Date

May 2018

Volume

278

Start / End Page

37 / 48

Related Subject Headings

  • Vitamin A
  • Up-Regulation
  • Skin Irritancy Tests
  • Skin
  • Silicones
  • Pharmacology & Pharmacy
  • Male
  • Keratin-19
  • Keratin-10
  • Humans
 

Citation

APA
Chicago
ICMJE
MLA
NLM
Shields, C. W., White, J. P., Osta, E. G., Patel, J., Rajkumar, S., Kirby, N., … Zauscher, S. (2018). Encapsulation and controlled release of retinol from silicone particles for topical delivery. Journal of Controlled Release : Official Journal of the Controlled Release Society, 278, 37–48. https://doi.org/10.1016/j.jconrel.2018.03.023
Shields, C Wyatt, John P. White, Erica G. Osta, Jerishma Patel, Shashank Rajkumar, Nickolas Kirby, Jean-Philippe Therrien, and Stefan Zauscher. “Encapsulation and controlled release of retinol from silicone particles for topical delivery.Journal of Controlled Release : Official Journal of the Controlled Release Society 278 (May 2018): 37–48. https://doi.org/10.1016/j.jconrel.2018.03.023.
Shields CW, White JP, Osta EG, Patel J, Rajkumar S, Kirby N, et al. Encapsulation and controlled release of retinol from silicone particles for topical delivery. Journal of controlled release : official journal of the Controlled Release Society. 2018 May;278:37–48.
Shields, C. Wyatt, et al. “Encapsulation and controlled release of retinol from silicone particles for topical delivery.Journal of Controlled Release : Official Journal of the Controlled Release Society, vol. 278, May 2018, pp. 37–48. Epmc, doi:10.1016/j.jconrel.2018.03.023.
Shields CW, White JP, Osta EG, Patel J, Rajkumar S, Kirby N, Therrien J-P, Zauscher S. Encapsulation and controlled release of retinol from silicone particles for topical delivery. Journal of controlled release : official journal of the Controlled Release Society. 2018 May;278:37–48.
Journal cover image

Published In

Journal of controlled release : official journal of the Controlled Release Society

DOI

EISSN

1873-4995

ISSN

0168-3659

Publication Date

May 2018

Volume

278

Start / End Page

37 / 48

Related Subject Headings

  • Vitamin A
  • Up-Regulation
  • Skin Irritancy Tests
  • Skin
  • Silicones
  • Pharmacology & Pharmacy
  • Male
  • Keratin-19
  • Keratin-10
  • Humans