Development and characterization of minoxidil-loaded liposomal system for delivery to pilosebaceous units.
The current study aimed to deliver minoxidil (2,4-diamino-6-piperidinopyrimidine 3-oxide; MXD), a potent hypertrichotic agent, into the pilosebaceous units, exploring the potential of the liposomal system. MXD-loaded liposomes of different compositions were prepared by a thin-film hydration technique and subsequently characterized for various vesicle-specific attributes (i.e., size, shape, lamellarity, and entrapment efficiency). Comparative analysis among these compositions was conducted with reference to their vesicle-specific parameters, drug deposition, and drug-delivery mechanism toward pilosebaceous units. The latter may bring about a distinct change in MXD therapy for various ailments related to pilosebaceous units, such as alopecia. The in vitro drug release, ex vivo skin permeation, and drug-retention behavior of the prepared formulation were evaluated by employing rat skin (normal as well as pilosebaceous free) and semipermeable membrane. The results revealed that the neutral liposomes (mean vesicle size, 3.83 +/- 0.18 microm) showed maximum drug deposition in the pilosebaceous units among all the other tested formulations. A quantitative estimation of pilosebaceous delivery revealed that the concentration of MXD in each pilosebaceous unit decreased in the following order: neutral liposomal formulation (5.8 x 10(3) to 7.25 x 10(3) microg) > positively charged liposomal formulation (4.7 x 10(3) to 5.87 x 10(3) microg) > negatively charged liposomal formulation (4.2 x 10(3) to 5.25 x 10(3) microg) > nonliposomal formulation (1.6 x 10(3) to 2.0 x 10(3) microg). Stability studies construed the need to store the liposomal formulation at lower temperatures. The results of the current work indicate that the neutral liposomes can deliver the drug molecules into pilosebaceous units more effectively than the other studied formulations.
Jain
Bhawna
B
University Institute of Pharmaceutical Sciences-UGC Center of Advanced Studies, Panjab University, Chandigarh, India.
Singh
Bhupinder
B
Katare
Om Prakash
OP
Vyas
Suresh Prashad
SP
D000818:Animals; D016503:Drug Delivery Systems; D008081:Liposomes / Q000737:chemistry*; D008914:Minoxidil / Q000008:administration & dosage*; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012627:Sebaceous Glands / Q000378:metabolism*
D008081:Liposomes; D008914:Minoxidil