ArticleInternational journal of nanomedicine2013
Optimized formulation of solid self-microemulsifying sirolimus delivery systems.
Article in International journal of nanomedicine, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Exploring novel type of lipid-bases drug delivery systems that contain one lipid and one water-soluble surfactant only.International journal of pharmaceutics · 2024Article
- Formulation and Evaluation of a Self-Microemulsifying Drug Delivery System of Raloxifene with Improved Solubility and Oral Bioavailability.Pharmaceutics · 2023Article
- Article
- High-Shear Wet Granulation of SMEDDS Based on Mesoporous Carriers for Improved Carvedilol Solubility.Pharmaceutics · 2022Article
- Supersaturation-Based Drug Delivery Systems: Strategy for Bioavailability Enhancement of Poorly Water-Soluble Drugs.Molecules (Basel, Switzerland) · 2022Review
- A comprehensive study of the basic formulation of supersaturated self-nanoemulsifying drug delivery systems (SNEDDS) of albendazolum.Drug delivery · 2021Article
- Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment.Pharmaceutics · 2020Article
- Solid Sirolimus Self-microemulsifying Drug Delivery System: Development and Evaluation of Tablets with Sustained Release Property.Iranian journal of pharmaceutical research : IJPR · 2019Article
- Use of Lipid Nanocarriers to Improve Oral Delivery of Vitamins.Nutrients · 2019Review
- Self-Emulsifying Granules and Pellets: Composition and Formation Mechanisms for Instant or Controlled Release.Pharmaceutics · 2017Review
- Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin.Molecules (Basel, Switzerland) · 2015Article
- Enhanced supersaturation and oral absorption of sirolimus using an amorphous solid dispersion based on Eudragit® e.Molecules (Basel, Switzerland) · 2015Article
- Preparation and in vivo evaluation of a dutasteride-loaded solid-supersaturatable self-microemulsifying drug delivery system.International journal of molecular sciences · 2015Article
- Design of a gelatin microparticle-containing self-microemulsifying formulation for enhanced oral bioavailability of dutasteride.Drug design, development and therapy · 2015Article
- Development of self-microemulsifying drug delivery system and solid-self-microemulsifying drug delivery system of telmisartan.International journal of pharmaceutical investigation · 2014Article
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundThe aim of this study was to develop an optimized solid self-microemulsifying drug delivery system (SMEDDS) formulation for sirolimus to enhance its solubility, stability, and bioavailability.
methodsExcipients used for enhancing the solubility and stability of sirolimus were screened. A phase-separation test, visual observation for emulsifying efficiency, and droplet size analysis were performed. Ternary phase diagrams were constructed to optimize the liquid SMEDDS formulation. The selected liquid SMEDDS formulations were prepared into solid form. The dissolution profiles and pharmacokinetic profiles in rats were analyzed.
resultsIn the results of the oil and cosolvent screening studies, Capryol™ Propylene glycol monocapry late (PGMC) and glycofurol exhibited the highest solubility of all oils and cosolvents, respectively. In the surfactant screening test, D-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) was determined to be the most effective stabilizer of sirolimus in pH 1.2 simulated gastric fluids. The optimal formulation determined by the construction of ternary phase diagrams was the T32 (Capryol™ PGMC:glycofurol:vitamin E TPGS = 30:30:40 weight ratio) formulation with a mean droplet size of 108.2 ± 11.4 nm. The solid SMEDDS formulations were prepared with Sucroester 15 and mannitol. The droplet size of the reconstituted solid SMEDDS showed no significant difference compared with the liquid SMEDDS. In the dissolution study, the release amounts of sirolimus from the SMEDDS formulation were significantly higher than the raw sirolimus powder. In addition, the solid SMEDDS formulation was in a more stable state than liquid SMEDDS in pH 1.2 simulated gastric fluids. The results of the pharmacokinetic study indicate that the SMEDDS formulation shows significantly greater bioavailability than the raw sirolimus powder or commercial product (Rapamune® oral solution).
conclusionThe results of this study suggest the potential use of a solid SMEDDS formulation for the delivery of poorly water-soluble drugs, such as sirolimus, through oral administration.
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