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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: 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 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.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

Scanning electron micrographs of (A) Aerosil® 200 and (B) SNEGs.Abbreviation: SNEGs, self-nanoemulsifying granules.
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f9-ijn-10-4459: Scanning electron micrographs of (A) Aerosil® 200 and (B) SNEGs.Abbreviation: SNEGs, self-nanoemulsifying granules.

Mentions: The scanning electron micrographs of Aerosil® 200 and CZL-loaded SNEGs are shown in Figure 9. Aerosil® 200 appeared as aggregates of rough surfaced amorphous particles. The SNEGs appeared as smooth surfaced nearly spherical particles, indicating that the liquid PCs are absorbed inside the pores of Aerosil® 200. No crystals were evident on the surface of the granules.


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)

Scanning electron micrographs of (A) Aerosil® 200 and (B) SNEGs.Abbreviation: SNEGs, self-nanoemulsifying granules.
© Copyright Policy
Related In: Results  -  Collection

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

f9-ijn-10-4459: Scanning electron micrographs of (A) Aerosil® 200 and (B) SNEGs.Abbreviation: SNEGs, self-nanoemulsifying granules.
Mentions: The scanning electron micrographs of Aerosil® 200 and CZL-loaded SNEGs are shown in Figure 9. Aerosil® 200 appeared as aggregates of rough surfaced amorphous particles. The SNEGs appeared as smooth surfaced nearly spherical particles, indicating that the liquid PCs are absorbed inside the pores of Aerosil® 200. No crystals were evident on the surface of the granules.

Bottom Line: 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 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.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