Development of liposome encapsulated clindamycin for treatment of acne vulgaris.
The enhancement of topical delivery of hydrophilic substances by use of multilammelar liposomes was measured ex vivo on pig ear skin and in vivo on hairless mice by electron paramagnetic resonance method (EPR). Multilamellar liposomes with different lipid composition (final concentration of membrane components is 48 mg/ml) were loaded with a hydrophilic spin probe GluSL, which does not penetrate the liposome membrane easily. They were characterized with respect to their stability, entrapped volume and enhancement characteristics. We observed significant differences in the properties of different types of liposomes with respect to their stability when in contact with the skin and their penetration into the skin. The results measured in vivo are consistent with those obtained ex vivo. On the basis of these findings the liposomes with appropriate stability and intradermal penetration characteristics were chosen for the development of liposome-encapsulated 1% clindamycin preparation for therapy of acne vulgaris. A double-blind clinical study was conducted to assess the safety and efficiency of liposome-encapsulated 1% clindamycin solution versus 1% clindamycin solution (Klimicin T, Lek). On the basis of the clinical trial it may be concluded that liposome-encapsulated 1% clindamycin solution was therapeutically superior over conventional 1% clindamycin solution in the treatment of acne vulgaris.
Honzak
L
L
University Medical Center, Nuclear Medicine Department, Ljubljana, Slovenia.
Sentjurc
M
M
D000152:Acne Vulgaris / Q000188:drug therapy*; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D002981:Clindamycin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D004311:Double-Blind Method; D006801:Humans; D008081:Liposomes; D051379:Mice; D008812:Mice, Hairless; D012867:Skin / Q000378:metabolism
D000900:Anti-Bacterial Agents; D008081:Liposomes; D002981:Clindamycin