Increased therapeutic efficacy of a newly synthesized tyrosinase inhibitor by solid lipid nanoparticles in the topical treatment of hyperpigmentation.

Abstract

Hyperpigmentation caused by melanin overproduction is a major skin disorder in humans. Inhibition of tyrosinase, a key regulator of melanin production, has been used as an effective strategy to treat hyperpigmentation. In this study, we investigated the use of solid lipid nanoparticles (SLNs) as a highly effective and nontoxic means to deliver a newly synthesized potent tyrosinase inhibitor, MHY498, and to target melanocytes through the skin. MHY498-loaded SLNs (MHY-SLNs) were prepared by an oil-in-water emulsion solvent-evaporation method, and their morphological and physicochemical properties were characterized. MHY-SLNs showed a prolonged drug-release profile and higher skin permeation than that of MHY solution. In an in vivo evaluation of antimelanogenic activity, MHY-SLNs showed a prominent inhibitory effect against ultraviolet B-induced melanogenesis, resulting in no change in the skin color of C57BL/6 mouse, compared with that observed in an MHY solution-treated group and an untreated control group. The antimelanogenic effect of MHY-SLNs was further confirmed through Fontana-Masson staining. Importantly, MHY-SLNs did not induce any toxic effects in the L929 cell line. Overall, these data indicate that MHY-SLNs show promise in the topical treatment of hyperpigmentation.

• Authors: Md Al-Amin, Jiafu Cao, Muhammad Naeem, Hasanul Banna, Min-Soo Kim, Yunjin Jung, Hae Young Chung, Hyung Ryong Moon, Jin-Wook Yoo
• Journal: Drug design, development and therapy (Drug Des Devel Ther) Vol. 10 Pg. 3947-3957 ( 2016) ISSN: 1177-8881 [Electronic] New Zealand
• PMID: 27980392 (Publication Type: Journal Article)

Chemical References

• (Z)-5-(2,4-dihydroxybenzylidene)thiazolidine-2,4-dione
• Drug Carriers
• Enzyme Inhibitors
• Lipids
• Melanins
• Thiazolidinediones
• Tyrosine 3-Monooxygenase

Topics

• Administration, Cutaneous
• Animals
• Cell Line
• Cell Survival (drug effects)
• Dose-Response Relationship, Drug
• Drug Carriers
• Drug Compounding
• Enzyme Inhibitors (administration & dosage, chemistry, pharmacology, toxicity)
• Fibroblasts (drug effects, pathology)
• Kinetics
• Lipids (chemistry)
• Melanins (metabolism)
• Mice, Inbred C57BL
• Nanoparticles
• Nanotechnology
• Permeability
• Skin (drug effects, enzymology, radiation effects)
• Skin Absorption
• Skin Pigmentation (drug effects)
• Solubility
• Technology, Pharmaceutical (methods)
• Thiazolidinediones (administration & dosage, chemistry, pharmacology, toxicity)
• Tyrosine 3-Monooxygenase (antagonists & inhibitors, metabolism)