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Preparation and evaluation of aceclofenac topical microemulsion.

Ramesh Shah R, Shripal Magdum C, Shivagonda Patil S, Shanawaj Niakwade N - Iran J Pharm Res (2010)

Bottom Line: Isopropyl myristate was chosen as the oil phase as it showed a good solubilising capacity.The mean diameters of the microemulsion droplets approximately ranged between 154 - 434 nm, and the permeability of aceclofenac incorporated into the microemulsion systems was 3 folds higher than that of the marketed formulation.These results indicate that the microemulsion system studied is a promising tool for percutaneous delivery of aceclofenac.

View Article: PubMed Central - PubMed

Affiliation: Appasaheb Birnale College of Pharmacy, Sangli, India.

ABSTRACT
A topical preparation containing aceclofenac was developed using an o/w microemulsion system. Isopropyl myristate was chosen as the oil phase as it showed a good solubilising capacity. Pseudo-ternary phase diagrams were used to obtain the concentration ranges of the oil, surfactant (Labrasol) and co-surfactant (plurol oleique) for microemulsion formation. Five different formulations were formulated with various amount of the oil (5-25%), water (10-50%), and the mixture of surfactant and co-surfactant at the ratio of 4 (45-65%). In vitro permeability of aceclofenac from the microemulsions was evaluated using Keshary Chien diffusion cells with 0.45-μm cellulose acetate membrane. The amount of the aceclofenac permeated was analyzed by HPLC and the droplet size and zeta potential of the microemulsions was determined using a Zetasizer Nano-ZS. The mean diameters of the microemulsion droplets approximately ranged between 154 - 434 nm, and the permeability of aceclofenac incorporated into the microemulsion systems was 3 folds higher than that of the marketed formulation. These results indicate that the microemulsion system studied is a promising tool for percutaneous delivery of aceclofenac.

No MeSH data available.


In vitro cumulative percent drug permeated from microemulsion formulations
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Figure 3: In vitro cumulative percent drug permeated from microemulsion formulations

Mentions: The drug permeation rates from various microemulsion formulations are illustrated in Figure 3. Amongst the formulations tested, the batch AILP – E showed the highest permeation rate (95.88%). The content of the surfactants mixture in microemulsions significantly affected the permeation rate of aceclofenac. As the content of the surfactants mixture was decreased from 65% to 45% at S/CoS = 4, the permeation rate of aceclofenac increased by 2 folds. This may be due to an increase in thermodynamic activity of the drug in the microemulsion at the lower content of surfactant, as aceclofenac is poorly water soluble and is solublised in the surfactant mixture (31). The results of the statistical tests also revealed that the formulation AILP – E showed a significant difference as compared to the marketed formulation (P< 0.05), while the other formulations showed no significant difference.


Preparation and evaluation of aceclofenac topical microemulsion.

Ramesh Shah R, Shripal Magdum C, Shivagonda Patil S, Shanawaj Niakwade N - Iran J Pharm Res (2010)

In vitro cumulative percent drug permeated from microemulsion formulations
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3869557&req=5

Figure 3: In vitro cumulative percent drug permeated from microemulsion formulations
Mentions: The drug permeation rates from various microemulsion formulations are illustrated in Figure 3. Amongst the formulations tested, the batch AILP – E showed the highest permeation rate (95.88%). The content of the surfactants mixture in microemulsions significantly affected the permeation rate of aceclofenac. As the content of the surfactants mixture was decreased from 65% to 45% at S/CoS = 4, the permeation rate of aceclofenac increased by 2 folds. This may be due to an increase in thermodynamic activity of the drug in the microemulsion at the lower content of surfactant, as aceclofenac is poorly water soluble and is solublised in the surfactant mixture (31). The results of the statistical tests also revealed that the formulation AILP – E showed a significant difference as compared to the marketed formulation (P< 0.05), while the other formulations showed no significant difference.

Bottom Line: Isopropyl myristate was chosen as the oil phase as it showed a good solubilising capacity.The mean diameters of the microemulsion droplets approximately ranged between 154 - 434 nm, and the permeability of aceclofenac incorporated into the microemulsion systems was 3 folds higher than that of the marketed formulation.These results indicate that the microemulsion system studied is a promising tool for percutaneous delivery of aceclofenac.

View Article: PubMed Central - PubMed

Affiliation: Appasaheb Birnale College of Pharmacy, Sangli, India.

ABSTRACT
A topical preparation containing aceclofenac was developed using an o/w microemulsion system. Isopropyl myristate was chosen as the oil phase as it showed a good solubilising capacity. Pseudo-ternary phase diagrams were used to obtain the concentration ranges of the oil, surfactant (Labrasol) and co-surfactant (plurol oleique) for microemulsion formation. Five different formulations were formulated with various amount of the oil (5-25%), water (10-50%), and the mixture of surfactant and co-surfactant at the ratio of 4 (45-65%). In vitro permeability of aceclofenac from the microemulsions was evaluated using Keshary Chien diffusion cells with 0.45-μm cellulose acetate membrane. The amount of the aceclofenac permeated was analyzed by HPLC and the droplet size and zeta potential of the microemulsions was determined using a Zetasizer Nano-ZS. The mean diameters of the microemulsion droplets approximately ranged between 154 - 434 nm, and the permeability of aceclofenac incorporated into the microemulsion systems was 3 folds higher than that of the marketed formulation. These results indicate that the microemulsion system studied is a promising tool for percutaneous delivery of aceclofenac.

No MeSH data available.