Using cyclodextrin complexation to enhance secondary photoprotection of topically applied ibuprofen.
Each year millions of people are overexposed to the sun resulting in photodamage of the skin. Secondary photoprotection is the application of medicinal agents to the body after sun exposure to reduce this damage. The objective of this study was to determine the affects of hydroxypropyl-beta-cyclodextrin (HPCD) complexation on the secondary photoprotective properties of topically applied ibuprofen. Complexation of ibuprofen by HPCD was demonstrated by differential scanning calorimetry, while solubilities were determined using HPLC. A linear (r2>0.999) relationship was found between ibuprofen solubility and HPCD concentration. For subsequent experiments, the concentration of ibuprofen was held constant at the solubility in 10% HPCD (10.6 mg/ml), while the HPCD concentration varied from 0 to 20% (w/w). In vitro transdermal permeation experiments demonstrated a parabolic relationship between transdermal kinetic parameters and HPCD concentration, with maximum values for both flux and skin accumulation occurring with the 10% HPCD formulation. In vivo experiments were performed by exposing hairless mice to UV radiation and applying ibuprofen-HPCD formulations topically at various times following UV exposure. Edema and epidermal lipid damage data demonstrated that application of ibuprofen-HPCD formulations within 1h of UV exposure provided significant photoprotection.
Godwin
Donald A
DA
College of Pharmacy, University of New Mexico Health Sciences Center, Albuquerque, NM 87131, USA. dgodwin@salud.unm.edu
Wiley
Cody J
CJ
Felton
Linda A
LA
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000287:Administration, Topical; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry*; D007052:Ibuprofen / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D066298:In Vitro Techniques; D008055:Lipids / Q000737:chemistry / Q000528:radiation effects; D051379:Mice; D008812:Mice, Hairless; D011837:Radiation-Protective Agents / Q000008:administration & dosage / Q000737:chemistry*; D012867:Skin / Q000187:drug effects / Q000378:metabolism / Q000528:radiation effects; D012869:Skin Absorption; D012995:Solubility; D013696:Temperature; D014466:Ultraviolet Rays; D047392:beta-Cyclodextrins / Q000737:chemistry*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D008055:Lipids; D011837:Radiation-Protective Agents; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D007052:Ibuprofen