Albumin coupled lipid nanoemulsions of diclofenac for targeted delivery to inflammation.
Diclofenac lipid nanoemulsions (DLNEs) were prepared with different compositions. Based on size, PDI, zeta potential, and in vitro drug release, the optimized DLNEs (DLNE-4 and DLNE-7) were developed and evaluated for drug content, entrapment efficiencies, and stability in comparison to the control formulation (DLNE-1). The albumin was coupled to DLNE-7 globules (DLNE-8) by water soluble carbodiimide (EDC) method, purified, and quantified by modified Bradford method. The pharmacokinetic study was conducted in inflammation (granuloma air pouch model) induced rats. The maximum peak concentration of DLNE-8 was almost fourfold to fivefold in comparison to drug solution in granuloma air pouch fluid (GAPF). The therapeutic availability (TA) of DLNE-8 was 2.89, 2.34, and 1.66 times that of drug solution, DLNE-4 and DLNE-7, respectively. The GAPF/serum ratio of diclofenac from DLNE-8 was above one at all time points indicating the targeting potential of albumin ligated LNEs to inflammatory sites.


BACKGROUND
This study demonstrates targeted delivery of diclofenac to an inflammatory environment using the granuloma air pouch model and diclofenac nanoemulsions with different compositions.
Nanotechnology Laboratory, Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Andhra Pradesh, India.
Prabhakar
P
Kandadi
Muzammil Afzal
MA
Syed
Surendar
S
Goparaboina
Kishan
K
Veerabrahma
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D002417:Cattle; D004008:Diclofenac / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D016503:Drug Delivery Systems; D004655:Emulsions / Q000737:chemistry*; D006099:Granuloma / Q000188:drug therapy* / Q000473:pathology; D007249:Inflammation / Q000188:drug therapy / Q000473:pathology; D008055:Lipids / Q000737:chemistry*; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D012710:Serum Albumin, Bovine / Q000737:chemistry*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004655:Emulsions; D008055:Lipids; D004008:Diclofenac; D012710:Serum Albumin, Bovine