Lipid-based capsaicin-loaded nano-colloidal biocompatible topical carriers with enhanced analgesic potential and decreased dermal irritation

Abstract

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.

Delivery of Thermoresponsive-Tailored Mixed Micellar Nanogel of Lidocaine and Prilocaine with Improved Dermatokinetic Profile and Therapeutic Efficacy in Topical Anaesthesia

“…All the animals in the respective groups were individually exposed to analgesiometer maintained at 55°C. As a standard protocol, the cut-off for the basal reaction time was fixed at 10 s. The reaction time was measured at various time intervals (15,30,45 and 60 min) for each group (38). The per cent analgesic effect was determined using Eq.…”

Capsaicin-loaded nanolipoidal carriers for topical application: design, characterization, and in vitro/in vivo evaluation

“…Nanolipoidal carriers (NLCs) are a promising type of topical drug carriers that can decrease dermal irritation 16 and be appropriate for application on injured or inflamed skin because they are based on nonirritant and nontoxic lipids. 17 Moreover, NLCs comprise solid and liquid lipids that lead to peculiar nanostructures with improved drug incorporation and release properties.…”

Novel elastic membrane vesicles (EMVs) and ethosomes-mediated effective topical delivery of aceclofenac: a new therapeutic approach for pain and inflammation

“…After application of formulation (0.5 g) on the tail of mice, the study was initiated. As a standard protocol, the cut-off for the basal reaction time was fixed as 10 s. The reaction time was measured at various time-intervals (15,30,45,60,90, and 120 min) for each group (Kulkarni, 1999;Raza et al, 2014b;Negi et al, 2015b). The percent analgesic effect was determined using the following equation: …”