21. June 2017
Candesartan cilexetil is an ester prodrug antagonist to angiotensin II receptor type 1 (AT1) used in management of many cardiovascular diseases. The absolute bioavailability of candesartan cilexetil is about (14–40%). Therefore, the paper aim was to prepare and evaluate solid self-nanoemulsifying drug delivery systems for candesartan cilexetil in order to improve its solubility, dissolution and stability.
01. March 2017
ABSTRACT Formulators face great challenges in adopting systematic approaches for designing self-nanoemulsifying formulations (SNEFs) for different drug categories. In this study, we aimed to build-up an advanced SNEF development framework for weakly basic lipophilic drugs, such as cinnarizine (CN). First, the influence of formulation acidification on CN solubility was investigated. Second, formulation self-emulsification in media with different pH was assessed. Experimentally designed phase...
09. May 2016
Aim The aim of this study is the development of self-emulsifying drug delivery systems (SEDDS) differing in amounts of ester substructures and to evaluate their stability in presence of pancreatic lipase and protective effect against luminal enzymatic metabolism using leuprorelin as model peptide drug. Methods Hydrophobic leuprolide oleate was incorporated into three different SEDDS formulations and their stability towards pancreatic lipases was investigated utilizing a dynamic in vitro...
02. March 2016
Oral administration is the most convenient way of all the drug delivery routes. Orally administered bioactive compounds must resist the harsh acidic fluids or enzyme digestion in stomach, to reach their absorbed destination in small intestine. This is the case for silibinin, a drug used to protect liver cells against toxins that has also been demonstrated in vitro to possess anti-cancer effects. However, as many other drugs, silibinin can degrade in the stomach due to the action of the gastric...
29. February 2016
The study investigated the use of monoacyl phosphatidylcholine (MAPC) in self-nanoemulsifying drug delivery system (SNEDDS). A D-optimal design was used to generate two sets of formulations containing long-chain (LC) or medium-chain (MC) glycerides, caprylocaproyl macrogol-8 glycerides (Labrasol), Lipoid S LPC 80 (LPC) (80% MAPC) and ethanol. The formulations were characterized using dynamic light scattering, microscopy, in vitro lipolysis and viscometric measurements. All LC formulations...