title: Evaluation of antinociceptive activity of nanoliposome-encapsulated and free-form diclofenac in rats and mice.
abstract: Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, antinociceptive, and antipyretic activities. Liposomes have been shown to improve the therapeutic efficacy of encapsulated drugs. The present study was conducted to compare the antinociceptive properties between liposome-encapsulated and free-form diclofenac in vivo via different nociceptive assay models. Liposome-encapsulated diclofenac was prepared using the commercialized proliposome method. Antinociceptive effects of liposome-encapsulated and free-form diclofenac were evaluated using formalin test, acetic acid-induced abdominal writhing test, Randall-Selitto paw pressure test, and plantar test. The results of the writhing test showed a significant reduction of abdominal constriction in all treatment groups in a dose-dependent manner. The 20 mg/kg liposome-encapsulated diclofenac demonstrated the highest antinociceptive effect at 78.97% compared with 55.89% in the free-form group at equivalent dosage. Both liposome-encapsulated and free-form diclofenac produced significant results in the late phase of formalin assay at a dose of 20 mg/kg, with antinociception percentages of 78.84% and 60.71%, respectively. Significant results of antinociception were also observed in both hyperalgesia assays. For Randall-Sellito assay, the highest antinociception effect of 71.38% was achieved with 20 mg/kg liposome-encapsulated diclofenac, while the lowest antinociceptive effect of 17.32% was recorded with 0 mg/kg liposome formulation, whereas in the plantar test, the highest antinociceptive effect was achieved at 56.7% with 20 mg/kg liposome-encapsulated diclofenac, and the lowest effect was shown with 0 mg/kg liposome formulation of 8.89%. The present study suggests that liposome-encapsulated diclofenac exhibits higher antinociceptive efficacy in a dose-dependent manner in comparison with free-form diclofenac.
authors: Department of Biomedical Sciences, Universiti Putra Malaysia, Serdang, Selangor, Malaysia.
authors: Jun Zheng
authors: JZ
authors: Goh
authors: Department of Biomedical Sciences, Universiti Putra Malaysia, Serdang, Selangor, Malaysia.
authors: Sook Nai
authors: SN
authors: Tang
authors: Department of Biomedical Sciences, Universiti Putra Malaysia, Serdang, Selangor, Malaysia ; InQpharm Group, Kuala Lumpur, Malaysia.
authors: Hoe Siong
authors: HS
authors: Chiong
authors: Department of Human Anatomy, Universiti Putra Malaysia, Serdang, Selangor, Malaysia.
authors: Yoke Keong
authors: YK
authors: Yong
authors: Department of Biomedical Sciences, Universiti Putra Malaysia, Serdang, Selangor, Malaysia.
authors: Ahmad
authors: A
authors: Zuraini
authors: Department of Biomedical Sciences, Universiti Putra Malaysia, Serdang, Selangor, Malaysia ; Halal Product Research Institute, Universiti Putra Malaysia, Serdang, Selangor, Malaysia.
authors: Muhammad Nazrul
authors: MN
authors: Hakim
mesh_terms: D019342:Acetic Acid / Q000633:toxicity; D000700:Analgesics / Q000008:administration & dosage / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000494:pharmacology; D002351:Carrageenan / Q000633:toxicity; D004008:Diclofenac / Q000008:administration & dosage / Q000494:pharmacology*; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D008081:Liposomes / Q000008:administration & dosage*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000008:administration & dosage*; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy*; D010147:Pain Measurement / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D008081:Liposomes; D004008:Diclofenac; D002351:Carrageenan; D019342:Acetic Acid
keywords: antinociceptive; diclofenac; efficacy; liposome; nanoencapsulation