Analgesic and anti-inflammatory controlled-released injectable microemulsion: Pseudo-ternary phase diagrams, in vitro, ex vivo and in vivo evaluation

Development of analgesic and anti-inflammatory controlled-released injectable microemulsions utilising lysine clonixinate (LC) as model drug and generally regarded as safe (GRAS) excipients. Different microemulsions were optimised through pseudo-ternary phase diagrams and characterised measuring dro...

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Bibliographic Details
Published in:European journal of pharmaceutical sciences 2017-04, Vol.101, p.220-227
Main Authors: Pineros, Isabel, Slowing, Karla, Serrano, Dolores R., de Pablo, Esther, Ballesteros, Maria Paloma
Format: Article
Language:English
Subjects:
Analgesic
Analgesics - administration & dosage
Analgesics - chemistry
Animals
Anti-inflammatory
Anti-Inflammatory Agents - administration & dosage
Anti-Inflammatory Agents - chemistry
Chemistry, Pharmaceutical - methods
Clonixin - administration & dosage
Clonixin - analogs & derivatives
Clonixin - chemistry
Controlled-release
Delayed-Action Preparations - administration & dosage
Delayed-Action Preparations - chemistry
Depot formulation
Drug Delivery Systems - methods
Drug Liberation
Emulsions - administration & dosage
Emulsions - chemistry
Excipients - chemistry
Humans
Injectable
Injections - methods
Injections, Intramuscular - methods
Lysine - administration & dosage
Lysine - analogs & derivatives
Lysine - chemistry
Lysine clonixinate
Male
Mice
Microemulsion
Particle Size
Polysorbates - chemistry
Pseudo-ternary diagrams
Rats
Rats, Wistar
Viscosity
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Summary:Development of analgesic and anti-inflammatory controlled-released injectable microemulsions utilising lysine clonixinate (LC) as model drug and generally regarded as safe (GRAS) excipients. Different microemulsions were optimised through pseudo-ternary phase diagrams and characterised measuring droplet size, viscosity, ex vivo haemolytic activity and in vitro drug release. The anti-inflammatory and analgesic activity was tested in mice (Hot plate test) and rats (Carrageenan-induced paw edema test) respectively and their activity was compared to an aqueous solution of LC salt. The aqueous solution showed a faster and shorter response whereas the optimised microemulsion increased significantly (p
ISSN:0928-0987
1879-0720
DOI:10.1016/j.ejps.2016.12.030