Nanoparticle Coated Submicron Emulsions: Sustained In-vitro Release and Improved Dermal Delivery of All-trans-retinol

• Published in: Pharmaceutical research Vol. 26; no. 7; pp. 1764 - 1775
• Main Authors: Ghouchi Eskandar, Nasrin, Simovic, Spomenka, Prestidge, Clive A
• Format: Journal Article
• Language: English
• Published: Boston Boston : Springer US 01-07-2009; Springer US; Springer; Springer Nature B.V
• Subjects: Administration, Cutaneous; all-trans-retinol; Animals; Biochemistry; Biological and medical sciences; Biomedical and Life Sciences; Biomedical Engineering and Bioengineering; Biomedicine; Drug Delivery Systems - methods; Emulsions - chemistry; General pharmacology; in-vitro release; Medical Law; Medical sciences; Nanoparticles; Nanoparticles - chemistry; Nanoparticles - ultrastructure; Pharmaceutical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Pharmacology/Toxicology; Pharmacy; Research Paper; Silica; silica nanoparticles; Silicon Dioxide - chemistry; Skin; Skin Absorption; skin penetration/permeation; submicron emulsion; Swine; Transdermal medication; Vitamin A - administration & dosage; Vitamin A - pharmacokinetics; all; retinol; submicron emulsion; skin penetration/permeation; release; silica nanoparticles; Pharmaceutical technology; Controlled release form; Nanoparticle; Permeation; In vitro; Silica; Retinol; Percutaneous route; Emulsion; Penetration; Dosage form; Microparticle; all-trans-retinol; Skin; Release; in-vitro release
• DOI: 10.1007/s11095-009-9888-0
• EISSN: 1573-904X
• ISSN: 0724-8741

Purpose The aim of this research is to investigate the dermal delivery of all-trans-retinol from nanoparticle-coated submicron oil-in-water emulsions as a function of the initial emulsifier type, the loading phase of nanoparticles, and the interfacial structure of nanoparticle layers. Methods The interfacial structure of emulsions was characterized using freeze-fracture-SEM. In-vitro release and skin penetration of all-trans-retinol were studied using Franz diffusion cells with cellulose acetate membrane, and excised porcine skin. The distribution profile was obtained by horizontal sectioning of the skin using microtome-cryostat and HPLC assay. Results The steady-state flux of all-trans-retinol from silica-coated lecithin emulsions was decreased (up to 90%) and was highly dependent on the initial loading phase of nanoparticles; incorporation from the aqueous phase provided more pronounced sustained release. For oleylamine emulsions, sustained release effect was not affected by initial location of nanoparticles. The skin retention significantly (p <= 0.05) increased and was higher for positive oleylamine-stabilised droplets. All-trans-retinol was mainly localized in the epidermis with deeper distribution to viable skin layers in the presence of nanoparticles, yet negligible permeation (~1% of topically applied dose) through full-thickness skin. Conclusions Sustained release and targeted dermal delivery of all-trans-retinol from oil-in-water emulsions by inclusion of silica nanoparticles is demonstrated.