Sustained-release diclofenac potassium-loaded solid lipid microparticle based on solidified reverse micellar solution: in vitro and in vivo evaluation

Objective: To formulate sustained-release diclofenac potassium-loaded solid lipid microparticles (SLMs) based on solidified reverse micellar solution (SRMS) and to evaluate the in vitro and in vivo properties. Methods: SRMS consisting of mixtures of Phospholipon® 90H and Softisan® 154 were used to f...

Full description

Saved in:
Bibliographic Details
Published in:Journal of microencapsulation 2013-01, Vol.30 (4), p.335-345
Main Authors: Chime, Salome Amarachi, Attama, Anthony Amaechi, Builders, Philip F., Onunkwo, Godswill C.
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics
Anti-Inflammatory Agents, Non-Steroidal - pharmacology
Biological and medical sciences
Diclofenac - chemistry
Diclofenac - pharmacokinetics
Diclofenac - pharmacology
diclofenac potassium
Drug Carriers - chemistry
Drug Carriers - pharmacokinetics
Drug Carriers - pharmacology
Drug Evaluation, Preclinical
Female
General pharmacology
Lipids - chemistry
Lipids - pharmacokinetics
Lipids - pharmacology
Male
Medical sciences
Micelles
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Rats
Rats, Wistar
SLMs
SRMS
sustained release
ulcerogenicity
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Objective: To formulate sustained-release diclofenac potassium-loaded solid lipid microparticles (SLMs) based on solidified reverse micellar solution (SRMS) and to evaluate the in vitro and in vivo properties. Methods: SRMS consisting of mixtures of Phospholipon® 90H and Softisan® 154 were used to formulate diclofenac potassium-loaded SLMs. Characterization based on the particle size and morphology, stability and encapsulation efficiency (EE%) were carried out on the SLMs. In vitro release was carried out in simulated intestinal fluid (pH 7.5). Anti-inflammatory and ulcerogenic properties were studied using rats. Results: Maximum EE% of 95%, 94% and 93% were obtained for SLMs formulated with SRMS 1:1, 2:1 and 1:2, respectively. In vitro release showed about 85-90% drug release at 13 h. Diclofenac potassium-loaded SLMs showed good anti-inflammatory and gastro-protective properties. Conclusion: Diclofenac potassium-loaded SLMs based on SRMS could be used orally or parenterally under controlled conditions, for once daily administration.
ISSN:0265-2048
1464-5246
DOI:10.3109/02652048.2012.726284