Salome A. Chime*, Paul A. Akpa, Cosmas C. Ugwuanyi and Anthony A. Attama Pages 1 - 11 ( 11 )
Background: Aspirin is a nonsteroidal anti-inflammatory drug that is very effective in the treatment of inflammation and other health conditions, however, it causes gastric irritation. Recently, researchers have developed patents (US9757529 2019) of inhalable aspirin for rapid absorption and circumvention of gastric irritation.
Aim: The aim of this work was to formulate aspirin-loaded lipid based formulation in order to enhance the oral bioavailability and inhibit gastric irritation.
Methods: This solid lipid microparticles loaded with aspirin (SLM) was formulated by modified cold homogenization-solvent evaporation method. In vitro studies such as in vitro drug release, particle size, encapsulation efficiency (EE), micromeritic properties and loading capacity were carried out. Pharmacodynamics studies such as anti-inflammatory and ulcerative properties of the SLM were also carried out in Wistar rats.
Results: The results showed that aspirin entrapped SLM exhibited highest EE of 72 % and particle size range of 7.60 ± 0.141µm to 20.25 ± 0.070 µm. Formulations had about 55 % drug release at 6 h in simulated intestinal fluid pH 6.8. The formulations had good flowability that could facilitate filling into hard gelatin capsule shells. The SLM exhibited 100 % gastroprotection against aspirin-induced ulcers (p < 0.05). The percentage anti-inflammatory activities also showed that aspirin-entrapped SLM had 78 % oedema inhibition at 7 h, while the reference had 68 % inhibition at 7 h.
Conclusion: Aspirin-entrapped SLM showed good sustained release properties, enhanced anti-inflammatory properties and total gastric protection from aspirin-induced ulcers and could be used as once daily oral aspirin.
Anti-Inflammatory, Aspirin, Drug Delivery, Gastroprotection, Kinetics Of Release, Lipids, Micromerics, Ulcers.Gugu
Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka 410001, Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka 410001, Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka 410001, Department of Pharmaceutics, University of Nigeria, Nsukka 410001