Crystal engineering, Bio Pharmaceutics and Cell biology of active pharmaceutical ingredient (drug) nanoparticles. Formation and cell interaction of hydrocortisone and prednisolone nanoparticles.

摘要

Nanotechnology applications have emerged enormously in recent times. Of particular interest is that area that overlaps the areas of nanotechnology, biology and medicine: nanomedicine. One advantage of nanomedicines is it that it can be used as an enabling technology by pharmaceutical researchers and industry to overcome issues associated with the low bioavailability of hydrophobic drugs. In the first part of the current study, nanosuspensions of two of hydrophobic steroid drugs: hydrocortisone and prednisolone were produced. Nanosuspensions were prepared using a bottom-up approach: the anti-solvent precipitation method using microfluidic reactors. Surface modification was carried out on these nanosuspensions using cationic surfactants to obtain nanoparticles with different levels of surface positive charge as indicated by ¿-potential values. Dynamic light scattering (DLS) and transmission electron microscope (TEM) techniques were used to characterize the prepared nanoparticles. Powder X-ray diffraction (PXRD) and differential scanning calorimetry (DSC) were also used to characterize hydrocortisone nanoparticles. In the second part, cellular uptake of both coated and uncoated nanoparticles by HaCaT keratinocytes cell line was examined and indicated by quantifying the anti- inflammatory effect of nanoparticles on the LPS-induced inflammation. Also, TEM was employed to evaluate the cellular uptake of hydrocortisone nanoparticles. Results showed higher ant-inflammatory effect of coated nanoparticles over uncoated nanoparticles. Furthermore, the anti-inflammatory effect of coated nanoparticles was correlated to the degree of positive surface charge.