Development of ciclopirox nail lacquer with enhanced permeation and retention.
Onychomycosis is a prevailing disease caused by fungal infection of nails that mostly affects athletes and the elderly. Ciclopirox is approved by the US Food and Drug Administration for the topical treatment of onychomycosis. However, the desired penetration of ciclopirox into the nail bed has not been achieved via topical application for efficient treatment. Therefore, the main aim of this study was to enhance ciclopirox permeation and retention in nail by the development of a new nail lacquer formulation. We screened the effects of different solvents, alkalizing agents, and permeation enhancers on the permeation of bovine hooves by ciclopirox and its retention in human nail clippings. The results suggest that isopropyl alcohol, potassium hydroxide, and urea as the solvent, alkalizing agent, and permeation enhancer, respectively, improved the permeation of the ciclopirox nail lacquer formulation the most with high flux rates. Comparison of the final formulation and marketed product revealed enhanced retention of ciclopirox from our developed formulation in human nail clippings. Therefore, our newly developed nail lacquer may be a potentially effective formulation for the treatment of onychomycosis in humans.
College of Pharmacy, Yeungnam University, 214-1 Dae-dong, Gyeongsan, 712-749, South Korea.
Raj Kumar
RK
Thapa
College of Pharmacy, Yeungnam University, 214-1 Dae-dong, Gyeongsan, 712-749, South Korea.
Ju Yeon
JY
Choi
College of Pharmacy, Yeungnam University, 214-1 Dae-dong, Gyeongsan, 712-749, South Korea.
Toe Gyung
TG
Go
Dong-A ST Research Institute, Pharmaceutical Product Research Laboratories, Yongin, 449-905, South Korea.
Min Hyung
MH
Kang
Dong-A ST Research Institute, Pharmaceutical Product Research Laboratories, Yongin, 449-905, South Korea.
Sang Duk
SD
Han
Dong-A ST Research Institute, Pharmaceutical Product Research Laboratories, Yongin, 449-905, South Korea.
Joon-Ho
JH
Jun
Dong-A ST Research Institute, Pharmaceutical Product Research Laboratories, Yongin, 449-905, South Korea.
Mi Won
MW
Son
College of Pharmacy, Yeungnam University, 214-1 Dae-dong, Gyeongsan, 712-749, South Korea.
Chul Soon
CS
Yong
College of Pharmacy, Yeungnam University, 214-1 Dae-dong, Gyeongsan, 712-749, South Korea. jongohkim@yu.ac.kr.
Jong Oh
JO
Kim
D000287:Administration, Topical; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000378:metabolism*; D002417:Cattle; D000077768:Ciclopirox; D006724:Hoof and Claw / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D007764:Lacquer; D009262:Nails / Q000187:drug effects / Q000378:metabolism*; D014009:Onychomycosis / Q000188:drug therapy / Q000378:metabolism; D010539:Permeability / Q000187:drug effects; D011728:Pyridones / Q000008:administration & dosage / Q000378:metabolism*
D000935:Antifungal Agents; D011728:Pyridones; D000077768:Ciclopirox
Ciclopirox; Nail lacquer; Onychomycosis; Potassium hydroxide; Urea