Lipid-based capsaicin-loaded nano-colloidal biocompatible topical carriers with enhanced analgesic potential and decreased dermal irritation.
Capsaicin (CP), a recent FDA-approved drug for the topical treatment of neuropathic pain, is associated with several side effects like irritation, burning sensation, and erythema, resulting in poor patient compliance. The present study is an attempt to study the effect of CP encasement in nano-lipoidal carriers (NLCs) on skin-transport characteristics, in vivo pharmacological performance, skin compliance, and stability of the finished product. The study also compares two methods of NLC preparation, namely microemulsification and rotary-evaporation for various attributes. The results demonstrated that microemulsion technique produced smaller nanoparticles vis-à-vis the rotary-evaporation method. Out of the various studied solid lipids, NLCs from stearic acid offered smallest size and the highest negative zeta potential. The NLC-gel offered higher skin permeation and skin retention of CP across LACA mice skin as compared with the conventional cream. The analgesic effect was observed to be enhanced substantially than that of the conventional cream when tested on a radiant mouse tail-flick model. The most alarming problems of skin-irritation and redness were successfully taken care by NLC-gel while the mice group receiving conventional cream showed marked changes in the skin histopathology. Besides the enhanced efficacy and decreased skin-irritation, the developed CP-NLCs also found to be stable and rheologically accepted formulation for the treatment of pain-associated disorders.
Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Study, Panjab University , Chandigarh , India .
Kaisar
K
Raza
Mohammad Afroz
MA
Shareef
Parteek
P
Singal
Gajanand
G
Sharma
Poonam
P
Negi
Om Prakash
OP
Katare
D000279:Administration, Cutaneous; D018712:Analgesics, Non-Narcotic / Q000008:administration & dosage* / Q000009:adverse effects / Q000378:metabolism / Q000627:therapeutic use; D000818:Animals; D002211:Capsaicin / Q000008:administration & dosage* / Q000009:adverse effects / Q000378:metabolism / Q000627:therapeutic use; D003102:Colloids; D004337:Drug Carriers / Q000008:administration & dosage* / Q000009:adverse effects / Q000378:metabolism / Q000627:therapeutic use; D004339:Drug Compounding; D005260:Female; D066298:In Vitro Techniques; D008081:Liposomes; D051379:Mice; D049329:Nanostructures / Q000737:chemistry*; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012869:Skin Absorption
D018712:Analgesics, Non-Narcotic; D003102:Colloids; D004337:Drug Carriers; D008081:Liposomes; D002211:Capsaicin
Analgesic; capsaicinoid; carbopol gel; radiant heat tail flick; rheology