Skin irritation and the inhibition effect on HSV-1 in vivo of penciclovir-loaded microemulsion.
The purpose of the present study was to investigate the skin irritation and pharmacodynamics of penciclovir-loaded microemulsion (PCV-ME). The formulation of PCV-ME was comprised of oleic acid (OA) (5%, w/w), Cremorphor EL (20%, w/w), ethanol (30%, w/w) and water (45%, w/w). PCV-ME presented as spherically shaped under transmission electron microscopy with an average diameter of 36.5 nm, and the solubility of PCV in microemulsion (ME) was 7.41 mg/g, almost 6 times that in water. Skin irritation test was performed in male guinea pigs, which demonstrated that no irritation effect was caused after single or multiple applications of PCV-ME. Likewise, male guinea pigs were employed as animal models which were infected with herpes simplex virus type 1 (HSV-1) in pharmacodynamics study. Real-time PCR was utilized to investigate the inhibition effect on HSV-1 exerted by commercial PCV-cream and PCV-ME. The results indicated that compared with commercial PCV-cream, PCV-ME could significantly inhibit the replication of HSV-1 in skin. In conclusion, PCV-ME could be a promising formulation which possessed the virtues of low irritation and high effectiveness.
Yu
Aihua
A
Department of Pharmaceutics, College of Pharmacy, Shandong University, Jinan 250012, China.
Guo
Chenyu
C
Zhou
Yabin
Y
Cao
Fengliang
F
Zhu
Weiwei
W
Sun
Min
M
Zhai
Guangxi
G
D000212:Acyclovir / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000737:chemistry / Q000627:therapeutic use; D000818:Animals; D000998:Antiviral Agents / Q000008:administration & dosage / Q000009:adverse effects* / Q000737:chemistry / Q000627:therapeutic use; D045744:Cell Line, Tumor; D004655:Emulsions; D006147:Guanine; D006168:Guinea Pigs; D006561:Herpes Simplex / Q000188:drug therapy* / Q000473:pathology; D018259:Herpesvirus 1, Human; D006801:Humans; D008297:Male; D012867:Skin / Q000473:pathology; D023422:Skin Irritancy Tests
D000998:Antiviral Agents; D004655:Emulsions; C053539:penciclovir; D006147:Guanine; D000212:Acyclovir