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Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication.

Sallam MA, Marín Boscá MT - Int J Nanomedicine (2015)

Bottom Line: The self-nanoemulsifying granules (SNEGs) filled into hard gelatin capsules showed two- and threefold increase in CZL released compared with conventional tablet and pure drug, respectively.The shelf life was 526 days at 25°C.Our study illustrated that the developed SNEGs, with bioenhancing ingredients, held great potential as a superior alternative to traditional oral formulations of CZL.

View Article: PubMed Central - PubMed

Affiliation: Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.

ABSTRACT
In this study, an optimized nanodispersible oral dosage form (containing a lactate ester) was developed for cilostazol (CZL). CZL is a phosphodiesterase inhibitor used for intermittent claudication. We aimed to improve the dissolution rate and absorption of CZL giving it a better chance of oral bioavailability, and to evaluate its stability on storage. Suitable compositions of nanoemulsion preconcentrate formulations were screened via solubility and compatibility tests. Response surface methodology and a desirability approach were applied to optimize preconcentrates containing minimum amount of surfactant mixture, maximum amount of lipid, and possessing the smallest globule size, with the highest emulsification and dissolution rates and minimum risk of drug precipitation. As part of the optimization process, the main effect, interaction effects and quadratic effects of amounts of lipid, and surfactant/co-surfactant ratio on % transmittance, globule size, emulsification time, drug precipitation, and drug release were investigated. The optimized formulation consisting of 28.9% butyl lactate, 28.9% Capryol, 27.82% Solubilisant Gamma 2429, and 14.18% Transcutol possessing a globule size of 60 nm was mixed with Aerosil 200. This gave uniform free flowing granules, which were characterized for surface and powder properties. The self-nanoemulsifying granules (SNEGs) filled into hard gelatin capsules showed two- and threefold increase in CZL released compared with conventional tablet and pure drug, respectively. The amount of drug permeated using non-everted sac technique from the SNEGs was twofold higher than that permeated from the tablet suspension. The shelf life was 526 days at 25°C. Our study illustrated that the developed SNEGs, with bioenhancing ingredients, held great potential as a superior alternative to traditional oral formulations of CZL.

No MeSH data available.


Related in: MedlinePlus

In vitro release profile of CZL from SNEGs, conventional tablet, and drug powder.Abbreviations: CZL, cilostazol; SNEGs, self-nanoemulsifying granules.
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f10-ijn-10-4459: In vitro release profile of CZL from SNEGs, conventional tablet, and drug powder.Abbreviations: CZL, cilostazol; SNEGs, self-nanoemulsifying granules.

Mentions: The in vitro dissolution profiles of SNEGs, pure CZL powder, and conventional tablets are shown in Figure 10. In case of pure drug powder, 278 mg SG was added to the dissolution medium. The dissolution profile of SNEGs filled in capsules showed a decrease in the rate of dissolution compared with the liquid PCs. A maximum of 82.42% of the drug was released after 45 minutes. This could be attributed to the additional disintegration step (time for the capsule to open) required for the drug dissolution, besides the time required for surfactant and co-surfactant to be released from the surface of silica. Some amount of surfactant and co-surfactant may also remain entrapped inside the granule. This may be the same reason for the observed increase in globule size of PCs after dispersing from SNEGs.


Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication.

Sallam MA, Marín Boscá MT - Int J Nanomedicine (2015)

In vitro release profile of CZL from SNEGs, conventional tablet, and drug powder.Abbreviations: CZL, cilostazol; SNEGs, self-nanoemulsifying granules.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4508069&req=5

f10-ijn-10-4459: In vitro release profile of CZL from SNEGs, conventional tablet, and drug powder.Abbreviations: CZL, cilostazol; SNEGs, self-nanoemulsifying granules.
Mentions: The in vitro dissolution profiles of SNEGs, pure CZL powder, and conventional tablets are shown in Figure 10. In case of pure drug powder, 278 mg SG was added to the dissolution medium. The dissolution profile of SNEGs filled in capsules showed a decrease in the rate of dissolution compared with the liquid PCs. A maximum of 82.42% of the drug was released after 45 minutes. This could be attributed to the additional disintegration step (time for the capsule to open) required for the drug dissolution, besides the time required for surfactant and co-surfactant to be released from the surface of silica. Some amount of surfactant and co-surfactant may also remain entrapped inside the granule. This may be the same reason for the observed increase in globule size of PCs after dispersing from SNEGs.

Bottom Line: The self-nanoemulsifying granules (SNEGs) filled into hard gelatin capsules showed two- and threefold increase in CZL released compared with conventional tablet and pure drug, respectively.The shelf life was 526 days at 25°C.Our study illustrated that the developed SNEGs, with bioenhancing ingredients, held great potential as a superior alternative to traditional oral formulations of CZL.

View Article: PubMed Central - PubMed

Affiliation: Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.

ABSTRACT
In this study, an optimized nanodispersible oral dosage form (containing a lactate ester) was developed for cilostazol (CZL). CZL is a phosphodiesterase inhibitor used for intermittent claudication. We aimed to improve the dissolution rate and absorption of CZL giving it a better chance of oral bioavailability, and to evaluate its stability on storage. Suitable compositions of nanoemulsion preconcentrate formulations were screened via solubility and compatibility tests. Response surface methodology and a desirability approach were applied to optimize preconcentrates containing minimum amount of surfactant mixture, maximum amount of lipid, and possessing the smallest globule size, with the highest emulsification and dissolution rates and minimum risk of drug precipitation. As part of the optimization process, the main effect, interaction effects and quadratic effects of amounts of lipid, and surfactant/co-surfactant ratio on % transmittance, globule size, emulsification time, drug precipitation, and drug release were investigated. The optimized formulation consisting of 28.9% butyl lactate, 28.9% Capryol, 27.82% Solubilisant Gamma 2429, and 14.18% Transcutol possessing a globule size of 60 nm was mixed with Aerosil 200. This gave uniform free flowing granules, which were characterized for surface and powder properties. The self-nanoemulsifying granules (SNEGs) filled into hard gelatin capsules showed two- and threefold increase in CZL released compared with conventional tablet and pure drug, respectively. The amount of drug permeated using non-everted sac technique from the SNEGs was twofold higher than that permeated from the tablet suspension. The shelf life was 526 days at 25°C. Our study illustrated that the developed SNEGs, with bioenhancing ingredients, held great potential as a superior alternative to traditional oral formulations of CZL.

No MeSH data available.


Related in: MedlinePlus