Effect of liposomes and niosomes on skin permeation of enoxacin.
The skin permeation and partitioning of a fluorinated quinolone antibacterial agent, enoxacin, in liposomes and niosomes, after topical application, were elucidated in the present study. In vitro percutaneous absorption experiments were performed on nude mouse skin with Franz diffusion cells. The influence of vesicles on the physicochemical property and stability of the formulations were measured. The enhanced delivery across the skin of liposome and niosome encapsulated enoxacin had been observed after selecting the appropriate formulations. The optimized formulations could also reserve a large amount of enoxacin in the skin. A significant relationship between skin permeation and the cumulative amount of enoxacin in the skin was observed. Both permeation enhancer effect and direct vesicle fusion with stratum corneum may contribute to the permeation of enoxacin across skin. Formulation with niosomes demonstrated a higher stability after 48 h incubation compared to liposomes. The inclusion of cholesterol improved the stability of enoxacin liposomes according to the results from encapsulation and turbidity. However, adding negative charges reduced the stability of niosomes. The ability of liposomes and niosomes to modulate drug delivery without significant toxicity makes the two vesicles useful to formulate topical enoxacin.
Fang
J Y
JY
Graduate Institute of Pharmaceutical Sciences, Taipei Medical University, 250 Wu-Hsing Street, Taipei, Taiwan. fajy@ms9.tisnet.tw
Hong
C T
CT
Chiu
W T
WT
Wang
Y Y
YY
D000279:Administration, Cutaneous; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002784:Cholesterol / Q000737:chemistry; D004337:Drug Carriers; D004339:Drug Compounding; D015365:Enoxacin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D005079:Excipients; D008081:Liposomes; D008863:Microspheres; D009391:Nephelometry and Turbidimetry; D012869:Skin Absorption
D000890:Anti-Infective Agents; D004337:Drug Carriers; D005079:Excipients; D008081:Liposomes; D015365:Enoxacin; D002784:Cholesterol