Permeability of olmesartan medoxomil from lipid based and suspension formulations using an optimized HDM-PAMPA model

English (OpenAlex)

Hexadecane membrane-parallel artificial membrane permeability assay (HDM-PAMPA) is based on an artificial HDM that separates the two compartments (donor and acceptor compartment). This model is used to predict the permeability of drugs in gastrointestinal tract and to simulate the passive absorption. In vivo behavior of the drugs can be estimated with these systems in drug development studies. In our study, we optimized HDM-PAMPA model to determine permeability of olmesartan medoxomil (OM) lipid based drug delivery system (OM-LBDDS). In order to prove that LBDDS formulation facilitates the weak permeability of OM, permeation rates were compared with the OM suspension formula (containing 0.25% v/w carboxymethylcellulose). The experiment was performed on a 96-well MultiScreen® PAMPA filter plate (MAIPN4510). The permeability of olmesartan formulations from the donor to acceptor compartment separated by a HDM membrane were determined by the previous validated HPLC method. We created positive control series without coating HDM to present the LBDDS and suspension formulation permeability from uncoated plates. The effective permeability constant (Pe) was calculated by the formula and improvement of permeability of OM-LBDDS formulation from HDM was confirmed. On the contrary there was no permeation of OM-Suspension in the hexadecane coated plates. As a result, the intestinal permeability of OM-LBDDS was calculated to be at least 100 times more than the suspension. OM-Suspension permeation was only observed in the hexadecane uncoated positive control plates. This was also manifestation of HDM-PAMPA mimicking permeability of intestines because of its lipidic construction.