Adv Pharm Bull. 2019;9(2):249-254.
doi: 10.15171/apb.2019.028
  Abstract View: 124
  PDF Download: 151

Research Article

Formulation and Physicochemical Characterization of Cyclosporine Microfiber by Electrospinning

Shahla Mirzaeei 1 ORCiD, Ghobad Mohammadi 1 * ORCiD, Navid Fattahi 2 ORCiD, Pardis Mohammadi 1 ORCiD, Ali Fattahi 1 ORCiD, Mohammad Reza Nikbakht 1 ORCiD, Khosro Adibkia 3 ORCiD

1 Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran.
2 Student Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran.
3 Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran

Abstract

Purpose: The objective of this study was to improve the permeability and water solubility rate of a poor water soluble drug, cyclosporine A (CsA).

Methods: In order to improve the drug dissolution rate and oral bioavailability, electrospinning method was used as an approach to prepare. The fibers were evaluated for surface morphology, thermal characterizations, drug crystallinity, in vitro drug release and in vivo bioavailability studies.

Results: Scanning electron microscope (SEM) results confirmed that the fibers were in microsize range and the size of the fibers was in the rang of 0.2 to 2 micron. Differential scanning calorimetry (DSC) and powder X-ray diffractometry (XRPD) analysis ensured that the crystalline lattice of drug were weakened or destroyed in the fibers. The drug release was 15.28%, 20.67%, and 32.84% from pure drug, fibers of formulation B, and formulation A, respectively. In vivo study results indicated that the bioavailability parameters of the optimized fiber formulation were improved and the maximum concentration (Cmax) were significantly higher for fibers (3001 ng/mL) than for pure drug (2550 ng/mL). The dissolution rate of the formulations was dependent on the nature and ratio of drug to carriers.

Conclusion: The physicochemical properties showed that the optimized mixture of polyethylene glycol (PEG) and povidone (PVP) fibers could be an effective carrier for CsA delivery. PEG and PVP fibers improved the absolute bioavailability and drug dissolution rate with appropriate physicochemical properties.

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Submitted: 09 Jan 2019
Revised: 28 Apr 2019
Accepted: 04 May 2019
First published online: 01 Jun 2019
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