Phospholipid microemulsion-based hydrogel for enhanced topical delivery of lidocaine and prilocaine: QbD-based development and evaluation

Drug Delivery

Sarwar Beg¹  Poonam Negi¹  Om Prakash Katare¹  Gajanand Sharma²  Bhupinder Singh³  Kaisar Raza⁴ 

[1] UGC Centre of Advanced Studies, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India;UGC Centre of Advanced Studies, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India;Department of Formulation Research, IPCA Laboratories Limited, Mumbai, Indi;UGC Centre of Advanced Studies, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India;UGC-Centre of Excellence in Nano Applications (Biomedical Sciences), Panjab University, Chandigarh, India an;UGC-Centre of Excellence in Nano Applications (Biomedical Sciences), Panjab University, Chandigarh, India an;

关键词: Analgesic;    eutectic mixture;    local anesthetic;    phospholipids;    skin-permeation;   

DOI  :  10.3109/10717544.2014.923067

来源: publisher

【 摘 要 】

Topical delivery of local anesthetics has been an area of interest for researchers considering the barrier properties of skin and unfavorable physicochemical properties of drugs. In the present study, efforts have been made to modify the in vivo efficacy of eutectic mixture of lidocaine and prilocaine by exploiting the phospholipid modified microemulsion based delivery systems. The strategic QbD (D-optimal mixture design) enabled systematic optimization approach, after having obtained the isotropic area of interest by ternary phase diagram, has resulted into the system with most desirable attributes. Latter include nano-scale, globular structures with an average size of 40.6 nm, as characterized by TEM and DLS. The optimized microemulsion systems in gel dosage forms revealed the better permeability over commercial cream (CC) through abdominal rat skin. Enhancement in the flux from MOPT-NMP gel was 3.22-folds for prilocaine and 4.94-folds for lidocaine, in comparison to that of CC. This enhanced skin permeability is very well reflected in the in vivo studies, wherein intensity and duration of action was augmented significantly. The skin compliance of the optimized formulation was revealed in histopathological studies. The overall benefit relating to efficacy and safety-compliance could be correlated to the uniqueness of the carriers, composed of phospholipids and other components. Hence, the developed phospholipid-microemulsion based gel formulation has been proposed as more useful alternative for the topical delivery of lidocaine and prilocaine.

【 授权许可】

Unknown