Continuous Production Of Raloxifene Hydrochloride Loaded Nanostructured Lipid Carriers Using Hot-Melt Extrusion Technology
Date of Award
M.S. in Pharmaceutical Science
Michael A. Repka
University of Mississippi
The aim of this study was to utilize a continuous process for the production of Raloxifene Hydrochloride (RX-HCl) loaded NLC formulations for extended drug release using hot-melt extrusion technology coupled with probe sonication, and also to evaluate the in vitro characteristics of the prepared NLCs by particle size, PDI, zeta potential, entrapment efficiency, drug loading, and in vitro drug release profile. Preparation of the NLCs using HME technology involved two main steps, first formation of a pre-emulsion after extrusion and then size reduction of the pre-emulsion using probe sonication to obtain the NLCs. Process parameters for the extrusion process like feeding rates for the volumetric feeder and peristaltic pumps, were optimized. A screw speed of 100 rpm and a barrel temperature of 85 °C, were used in the extrusion process. Characterization of the NLCs involved assessment of particle size, PDI, zeta potential, entrapment efficiency, and drug loading. NLCs prepared by HME technology generally shoa lower particle size compared to those prepared by the conventional method. The prepared NLCs had high entrapment efficiency values (>90 %). In vitro drug release was evaluated using dialysis bag diffusion technique and USP apparatus 1 (rotating basket). The pure drug shoa faster rate of drug release compared to the NLCs which shoan extended release of the drug. NLCs prepared by HME technology generally shoa higher rate of drug release compared to those prepared by the conventional method. Particle size of the prepared NLCs remained relatively stable over the storage period and all PDI and zeta potential values were ≤ 0.523 and in the range of -15 to -30 mV, respectively, indicating good physical stability of the formulations. In summary, HME technology and probe sonication were successfully used to prepare RX-HCl loaded NLC formulations as a continuous manufacturing process with shorter processing times as compared to the conventional method, which makes this technique a more industry friendly method.
Muhindo, Derick, "Continuous Production Of Raloxifene Hydrochloride Loaded Nanostructured Lipid Carriers Using Hot-Melt Extrusion Technology" (2019). Electronic Theses and Dissertations. 1935.