Deposition of salicylic acid into hamster sebaceous.
In an earlier paper, we identified vehicles that are miscible with sebum, using differential scanning calorimetry (DSC). In this paper, the potential of these vehicles to deliver salicylic acid (SA) into the sebum-filled follicles of hamster ears is examined. The main objective of this study is to correlate the melting transitions of a model sebum with the follicular delivery of SA, using two different types of vehicles (fatty and polar). Generally, the fatty vehicles show higher deposition than the polar vehicles. Follicular delivery of salicylic acid correlates well with its solubility in the respective vehicles. This extent of deposition also shows a relationship with the effect of the vehicle on thermal behavior of the model sebum. The nature of the relationship depends on the vehicle (polar or fatty) tested. We conclude that DSC could be used to identify appropriate vehicles for drugs whose follicular delivery depends on solubility. The results also suggest that delivery into the sebaceous glands occurs by two different mechanisms, depending upon the polarity of the vehicle and the physicochemical properties of the drug. The results of these experiments are further extended to investigate follicular delivery of SA from two different types of oil-in-water emulsion formulations. From these studies we conclude that either increasing the volume of the oil phase or changing the emulsion to a water-in-oil emulsion would increase follicular deposition. Our research highlights the role of sebum, its compatibility with drug molecules, and vehicle selection in the transport of drugs into the follicles. The overall results of these experiments provide a reasonable understanding of the mechanisms underlying the transport of drugs to, and subsequently through, the sebaceous follicle.
Motwani
M R
MR
Department of Pharmaceutics, College of Pharmacy,Rutgers University, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA.
Rhein
L D
LD
Zatz
J L
JL
D000818:Animals; D002152:Calorimetry, Differential Scanning; D006224:Cricetinae; D004423:Ear; D045703:Emulsifying Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D004655:Emulsions; D018859:Hair Follicle / Q000502:physiology; D066298:In Vitro Techniques; D008297:Male; D008647:Mesocricetus; D020156:Salicylic Acid / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D012627:Sebaceous Glands / Q000378:metabolism*; D012629:Sebum / Q000737:chemistry / Q000378:metabolism*
D045703:Emulsifying Agents; D004655:Emulsions; D020156:Salicylic Acid