Oral Bioavailability Enhancement of Exemestane from Self-Microemulsifying Drug Delivery System (SMEDDS)

Singh, Ajeet; Chaurasiya, Akash; Awasthi, Anshumali; Mishra, Gautam; Asati, Dinesh P; Khar, Roop K.; Mukherjee, Rama

doi:10.1208/s12249-009-9281-7

Cited by 123 publications

(62 citation statements)

References 33 publications

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“…The resulting emulsions were stored for 12 h at room temperature and demonstrated for any signs of phase separation or drug precipitation. [35] Thermodynamic stability studies Nateglinide loaded SEDDS were diluted with purified water and centrifuged at 3500 rpm for 30 min and then checked for instability such as phase separation, creaming or cracking. Freeze-thaw cycle was carried out at −21°C and +25°C, which involved three cycles with storage at each temperature for not <48 h.…”

Section: Robustness To Dilutionmentioning

confidence: 99%

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Suvarna

2017

AJP

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Introduction: To develop self-emulsifying drug delivery system (SEDDS) of nateglinide to convert it into solid SEDDS (S-SEDDS) aerosil-200 as adsorbent. Materials and Methods: Nateglinide solid self-micro emulsifying drug delivery system (S-SMEDDS) formulation was prepared by adsorption to solid carrier technique, where the liquid SMEDDS are allowed to adsorb onto the surface of free flowing aerosil-200. Solubility study, ternary phase diagram, robustness to dilution, viscosity determination, cloud point measurement, thermodynamic stability study, and globule size analysis were adopted to optimize liquid SEDDS. S-SEDDS were evaluated for various studies including in vivo study. The optimized liquid SEDDS formulation consisted of nateglinide, capyrol-90, tween 80, Transcutol P. Results: The results of this study suggest the potential use of developed S-SEDDS formulation for the delivery of poorly water-soluble drug nateglinide. Conclusion: The developed S-SMEDDS is a promising strategy for solubility enhancement of poorly water-soluble drug nateglinide.

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Section: Robustness To Dilutionmentioning

confidence: 99%

Untitled

Suvarna

2017

AJP

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“…labrasol and transcutol were used as the surfactant/cosurfactant system and were employed at a ratio of 1:1 w/w (Singh et al, 2009). Mixtures of oil with surfactant or surfactant-cosurfactant system was prepared at ratios of 1:19, 2:18, 2.5:17.5, 3:17, 3.5:16.5, 4:16, 4.5:15.5, 5:15, 5.5:14.5, 6:14, 8:12 and 10:10; oil to surfactant system respectively.…”

Section: Determination Of Phase Behaviormentioning

confidence: 99%

“…Based on the results of this solubility and the miscibility of the surfactant cosurfactant system with the castor oil, the components of SEDDS were castor oil with labrasol and transcutol. Similar components were successfully used to prepare SEDDS containing castor oil (Singh et al, 2009). Determination of the phase behavior SEDDS should form emulsions or microemulsions under the gentle agitation of the digestive motility in the stomach and intestines.…”

Section: Solubility Screeningmentioning

confidence: 99%

Self microemulsefying and non-self microemulsefying liquisolid tablet of felodipine

Khorshed¹,

Maghraby²

2016

J App Pharm Sci

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Liquisolid formulation involves dissolution or dispersion of the drug in a liquid before formulation of solid dosage form using solid adsorbent as a carrier. The liquid component usually utilizes simple solvent system. Self emulsifying liquids can provide another alternative liquid for enhanced dissolution. The objective of this work was to develop and evaluate non-self emulsifying and self emulsifying liquisolid tablet for enhanced dissolution rate of felodipine. The former utilized polyethylene glycol 400 which was the best solvent and the later employed a mixture of castor oil with labrasol and transcutol as self emulsifying system. A mixture of avicel PH 102 and aerosil 200 was used as solid adsorbent with croscarmellose being used as superdisintegrent. Formulation of the drug as liquisolid tablets enhanced the dissolution rate compared with the standard tablet prepared using the unprocessed drug powder with the same tablet excipients. The self emulsifying tablet showed faster release pattern compared with the non-self emulsifying tablet. The thermal analysis studies indicated the presence of the drug in a solution form in the tablet formulations. In conclusion liquisolid tablet formulation can enhance the dissolution rate of felodipine with self emulsifying liquid system being more efficient.

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“…Visual clarity of the prepared 15 formulations (F1-F15) was performed against black and white background and further the turbidity of batches was verified as per the method described by Singh et al 16 …”

Section: Appearancementioning

confidence: 99%

Design and evaluation of solid self-emulsifying drug delivery system of rosuvastatin calcium

Rokad¹,

Nagda²,

Nagda³

2014

J. Young Pharm.

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Background:The work has been undertaken with an objective to prepare a self-emulsifying drug delivery system (SEDDS) of rosuvastatin calcium (ROS) with the least amount of surfactant which could enhance its solubility and oral bioavailability. Materials and Methods: Spectrophotometric method was used to estimate the solubility of the drug in various oils, surfactant and co-surfactant. The phase behavior and most efficient self-emulsifying region were identified by constructing pseudo ternary phase diagram. The solid-SEDDS (S-SEDDS) was prepared using an adsorbent consequently the prepared S-SEDDS were filled up in hard gelatin capsule which were evaluated for various physicochemical parameters. Results: The composition of optimized formulation consisted of 10 mg of ROS, capmul MCM (oil), cremophor ELP (surfactant) and propylene glycol (co-surfactant). The optimized formulation showed negative zeta potential (−22.11 mv), optimal particle size (10.59 nm) and demonstrated excellent self-emulsifying ability with a maximum solubilizing capability. The S-SEDDS formulations were prepared from the optimized liquid SEDDS, which revealed maximum release rate (97.7%) among all the prepared S-SEDDS formulation and marketed formulation. Conclusion: It was concluded that S-SEDDS prepared from liquid SEDDS can be a promising novel approach to enhance the solubility and drug release of ROS, which in turn also develops a stable formulation, least drugs leakage and precipitation than the liquid SEDDS.

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Oral Bioavailability Enhancement of Exemestane from Self-Microemulsifying Drug Delivery System (SMEDDS)

Cited by 123 publications

References 33 publications

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Self microemulsefying and non-self microemulsefying liquisolid tablet of felodipine

Design and evaluation of solid self-emulsifying drug delivery system of rosuvastatin calcium

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