J Appl Biomed 14:147-155, 2016 | DOI: 10.1016/j.jab.2015.11.001

Quasi emulsion spherical crystallization technique based environmentally responsive Tulsion® (pH dependent) microspheres for colon specific delivery

Ashish Jaina,*, Ankit Jaina, Abhishek Jainb, Anki Jainb
a Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar 470 003, India
b Sagar Institute of Pharmaceutical Sciences, Sagar 470 228, India

pH-dependent sustained-release Tulsion® microspheres bearing clarithromycin were prepared using quasi-emulsion solvent diffusion method with thermocoat L 30 D 55 as a release retardant. Both, clarithromycin and thermocoat L 30 D 55, were found to be non-hemolytic during in vitro toxicity assay against human red blood cells. Ratiometric optimization of different solvents using phase diagrams was performed on amount of good solvent, bridging liquid, dispersing liquid and poor solvent. The developed microspheres were evaluated for the recovery (67.27 ± 3.3%), average particle size (52.0 ± 0.46 μm) and encapsulation efficiency (61.0 ± 3.1%). Scanning electron microscopy and transmission electron microscopy revealed that the microspheres were smooth in surface and spherical in shape, respectively. The drug release study was conducted at different pH of GIT and it gave a pH dependent release for clarithromycin. The bioavailability study revealed increased AUC (2 fold) and half-life (1.2 fold) of microspheres as compared to plain drug. The manuscript reported the debut work on thermocoat L 30 D 55 based novel drug delivery system, the polymer is safe to be used, quasi emulsion spherical crystallization technique is a good technique to prepare microspheres, the prepared microspheres provides sustain release profile as well as targeting to colon.

Keywords: Spherical crystallization technique; Clarithromycin; Sustained-release microspheres; Quasi-emulsion solvent diffusion method; Tulsion® (thermocoat L 30 D 55); Methacrylic acid copolymer (type-C)

Received: July 22, 2015; Revised: October 28, 2015; Accepted: November 2, 2015; Published: April 1, 2016  Show citation

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Jain A, Jain A, Jain A, Jain A. Quasi emulsion spherical crystallization technique based environmentally responsive Tulsion® (pH dependent) microspheres for colon specific delivery. J Appl Biomed. 2016;14(2):147-155. doi: 10.1016/j.jab.2015.11.001.
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