Graduation Year

2021

Document Type

Thesis

Degree

M.S.

Degree Name

Master of Science (M.S.)

Degree Granting Department

Graduate School

Major Professor

Vijay Kumar Sutariya, Ph.D.

Co-Major Professor

Sheeba Varghese Gupta, M. Pharm, Ph.D.

Committee Member

Pranav Patel, Ph.D.

Committee Member

Feng Cheng, Ph.D.

Keywords

Nanostructured Lipid Carriers, Permeability, Raloxifene, Sustained Release

Abstract

Raloxifene (RLX), a BCS class-II drug is a selective estrogen receptor modulator (SERM)having estrogenic effect on bone and antiestrogenic effect on endometrium and breast respectively. Low solubility, high permeability, high metabolism and low bioavailability are the characteristics of raloxifene. It is used to prevent and treat in women and those on It is also used to reduce the risk of in those at high risk. Although 60% is absorbed orally, raloxifene shows extremely poor bioavailability (2%) owing to its low solubility and an extensive (>90%) intestinal/hepatic first-pass metabolism. Hence it becomes important to increase the solubility of raloxifene in order to enhance its bioavailability. In this study, Raloxifene nanostructured lipid carriers (RNLCs) were successfully prepared using melt dispersion ultrasonication method. The prepared RNLCs were characterized and the in-vitro studies were carried out in the human epithelial breast cancer cell line (MCF-7 cell line). The RNLCs have a size of 114.8±0.98 nm and zeta potential of +9.21±0.58 mV. TEM images showed the particle size ranging from 65nm to 120nm. With an entrapment efficiency of 75.04%±2.75%, the RNLCs showed sustained release over seven days’ time compared to 24 hours for raloxifene drug solution. The prepared RNLCs were successfully take up by the MCF-7 cells in time dependent manner and the RNLCs showed decreased cell viability compared to raloxifene drug. This suggests the RNLCs were more potent than the raloxifene drug. Using the PAMPA, the permeability rate for raloxifene solution was calculated to be 8X10?6 cm/s and for the RNLCs it was calculated to be 17.8X10?6 cm/s. Hence, from the Permeability rate calculated, we can conclude that raloxifene when formulated as NLCs have increased permeability. Overall, the prepared RNLCs were found to be superior than the raloxifene drug as such.

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