Design of cissus-alginate microbeads revealing mucoprotection properties in anti-inflammatory therapy.
Cissus gum has been employed as polymer with sodium alginate in the formulation of diclofenac microbeads and the in vivo mucoprotective properties of the polymer in anti-inflammatory therapy assessed in rats with carrageenan-induced paw edema in comparison to diclofenac powder and commercial diclofenac tablet. A full 2(3) factorial experimental design has been used to investigate the influence of concentration of cissus gum (X1); concentration of calcium acetate (X2) and stirring speed (X3) on properties of the microbeads. Optimized small discrete microbeads with size of 1.22±0.10 mm, entrapment efficiency of 84.6% and t80 of 15.2±3.5 h were obtained at ratio of cissus gum:alginate (1:1), low concentration of calcium acetate (5% w/v) and high stirring speed (400 rpm). In vivo studies showed that the ranking of percent inhibition of inflammation after 3h was diclofenac powder>commercial tablet=cissus>alginate. Histological damage score and parietal cell density were lower while crypt depth and mucosal width were significantly higher (p<0.05) in the groups administered with the diclofenac microbeads than those administered with diclofenac powder and commercial tablet, suggesting the mucoprotective property of the gum. Thus, cissus gum could be suitable as polymer in the formulation of non-steroidal anti-inflammatory drugs ensuring sustained release while reducing gastric side effects.
Department of Pharmaceutics & Industrial Pharmacy, University of Ibadan, Ibadan, Nigeria.
Adenike
A
Okunlola
Department of Pharmaceutics & Industrial Pharmacy, University of Ibadan, Ibadan, Nigeria; Laboratory of Pharmaceutical Technology, Institute of Pharmacy, Rheinische Friedrich-Wilhelms University, Bonn, Germany. Electronic address: pejuodeku@yahoo.com.
Oluwatoyin A
OA
Odeku
Laboratory of Pharmaceutical Technology, Institute of Pharmacy, Rheinische Friedrich-Wilhelms University, Bonn, Germany.
Alf
A
Lamprecht
Department of Veterinary Physiology, Biochemistry and Pharmacology, University of Ibadan, Ibadan, Nigeria.
Ademola A
AA
Oyagbemi
Department of Veterinary Physiology, Biochemistry and Pharmacology, University of Ibadan, Ibadan, Nigeria.
Olayinka A
OA
Oridupa
Department Veterinary Anatomy, University of Ibadan, Ibadan, Nigeria.
Oluwasanmi O
OO
Aina
D000085:Acetates / Q000737:chemistry; D000464:Alginates / Q000737:chemistry*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology*; D017610:Calcium Compounds / Q000737:chemistry; D002351:Carrageenan; D003692:Delayed-Action Preparations; D004008:Diclofenac / Q000737:chemistry / Q000494:pharmacology*; D004339:Drug Compounding; D065546:Drug Liberation; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology; D005163:Factor Analysis, Statistical; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D006614:Hindlimb; D007700:Kinetics; D008297:Male; D008863:Microspheres; D010316:Particle Size; D053149:Plant Gums / Q000737:chemistry*; D051381:Rats; D013270:Stomach / Q000187:drug effects
D000085:Acetates; D000464:Alginates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D017610:Calcium Compounds; C429904:Cissus stem gum; D003692:Delayed-Action Preparations; D006603:Hexuronic Acids; D053149:Plant Gums; D004008:Diclofenac; D020723:Glucuronic Acid; D002351:Carrageenan; C120662:calcium acetate
Cissus gum; Microbeads; Mucoprotective properties