Abstract
Solid lipid microparticles (SLMs) represent an alternative carrier system to traditional colloidal carrier such as emulsion, liposomes and polymeric micro and nanoparticles. The purpose of this research work was to develop and evaluate solid lipid microparticles of sirolimus for oral delivery. Sirolimus is an immunosupressive drug used to prevent transplant rejection and to treat auto immune diseases. It is a macrolide lactone produced by streptomyces hydroscopicus . It is extremely hydrophobic. Sirolimus solid lipid microparticles were prepared by hot homogenization technique. The matrix chiefly consisted of glyceryl monostearate and sodium taurocholate. The SLMs were studied for its particle size analysis, drug content, entrapment efficiency, in vitro release characteristics and also for stability analysis at different temperature and humidity conditions. Average particle size was found to be 21.40μm. Drug content of SLMs determined by HPLC analysis was found to be 98.6±0.31% while entrapment efficiency achieved was 98.02%. Drug release from the final formulation was found to be 90.3% in 90 min. SLMs formulated with glyceryl monostearate and sodium taurocholate can be used for oral delivery of hydrophobic drugs with in-vivo study still to be explored.
Highlights
Sirolimus (Rapamycin, Rapammune) is a macrolide lactone produced by streptomyces hydroscopicus
Sirolimus has a novel mechanism of immunosuppressant action involving the suppression of T-lymphocyte proliferation through inhibition of the target of rapamycin protein kinase complex (TORC) [4]
The formulations were optimized by first preparing blank microparticles by varying the content of glyceryl monostearate (GMS) and sodium taurocholate and by varying the processing parameters as shown in Table 1 and 2
Summary
Sirolimus (Rapamycin, Rapammune) is a macrolide lactone produced by streptomyces hydroscopicus. It is an immunosupressive agent used for the prophylaxis of renal allograft rejection. The drug was first isolated from a soil sample from Rapa Nui, an island in the south pacific, the prefix “Rapa”. It is extremely hydrophobic having molecular weight 914.2 g/mol [1,2,3]. Sirolimus has a novel mechanism of immunosuppressant action involving the suppression of T-lymphocyte proliferation through inhibition of the target of rapamycin protein kinase complex (TORC) [4]. Blockade of TORC inhibits cytokine-mediated proliferation in T cells, B cells and mesenchymal cells, including smooth muscle cells [5]
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