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Related Experiment Video

Updated: May 20, 2026

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles

Published on: August 28, 2015

Sirolimus solid self-microemulsifying pellets: formulation development, characterization and bioavailability

Xiongwei Hu¹, Chen Lin, Dingxiong Chen

¹Department of Pharmacy, Fuzhou General Hospital of Nanjing Military Region, Fuzhou 350025, China.

International Journal of Pharmaceutics

|August 2, 2012

Summary

This summary is machine-generated.

Developing self-microemulsifying drug delivery systems (SMEDDS) pellets improved sirolimus (SRL) oral absorption. These SRL-SMEDDS pellets demonstrated enhanced redispersion and bioavailability compared to commercial tablets.

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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

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Last Updated: May 20, 2026

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles

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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Published on: July 27, 2022

Area of Science:

Pharmaceutical Technology
Drug Delivery Systems
Biopharmaceutics

Background:

Sirolimus (SRL), a water-insoluble drug, exhibits poor oral absorption.
Enhancing dissolution and bioavailability is crucial for effective SRL therapy.

Purpose of the Study:

To develop and evaluate self-microemulsifying pellets of sirolimus (SRL-SMEDDS).
To improve the oral absorption and dissolution of sirolimus.
To assess the feasibility of the extrusion-spheronization method for solidifying liquid SMEDDS.

Main Methods:

Screening and optimization of liquid SRL-SMEDDS using solubility tests, self-emulsifying grading, ternary phase diagrams, and central composite design.
Preparation of SRL-SMEDDS pellets via extrusion-spheronization.
Evaluation of pellet characteristics including redispersion, droplet size, polydispersity index, size, friability, and drug crystallinity (DSC, XRPD, IR).
Pharmacokinetic study in beagle dogs comparing SRL-SMEDDS pellets to commercial SRL tablets (Rapamune).

Main Results:

The optimal SRL-SMEDDS pellet formulation was determined.
SRL-SMEDDS pellets exhibited significantly faster redispersion rates than commercial SRL tablets.
Solidification did not adversely affect microemulsion droplet size or polydispersity index.
Pellet size and friability met quality standards, with no crystalline sirolimus detected.
Oral relative bioavailability of SRL-SMEDDS pellets was approximately 136.9% compared to Rapamune.

Conclusions:

Solid self-microemulsifying drug delivery system (SMEDDS) pellets represent a promising strategy for enhancing sirolimus oral absorption.
The extrusion-spheronization technique is a viable method for solidifying liquid SMEDDS formulations.