The effect of intestinal bile on the stability of lipid-based vesicular system used as oral drug carriers
نویسنده
چکیده
Received: December 02, 2016; Accepted: December 21, 2016; Published: December 23, 2016 Intestinal bile salts are bio-surfactants existing in the gastrointestinal tract (GIT) which have essential role either on fat and lipid digestion or absorption [1]. Acidic lipases, which are secreted by the gastric chief cells in the fundic mucosa of the stomach, regulate10-30% of the lipid hydrolysis. In the other hand, pancreatic lipases make up to 90% of lipid hydrolysis in the small intestine. The process is supported by bile salts distributed through a network of bile ducts, first secreted from hepatocytes, transported viabile canaliculi, exit the liver via hepatic duct, joined with cystic and pancreatic duct to finally enter the small intestine. This hepatic bile contains large quantities of bile acids, cholesterol and other organic molecules. The main function of bile salt is to enhance emulsification and absorption of oils and lipoids upon aggregations. Thus, intestinal bile salts have an immediate effect on the lipolysis process of lipid-based components [2]. Similarly, lipidbased colloidal systems used for oral drug delivery system such as liposomes are expected to be subjected to these digestion processes. Being highly susceptible to the detergent effect of intestinal bile salt they tend to undergo destruction of the phospholipids bilayer and ultimately the solubilisation of the vesicular membrane [3]. As a result of the solubilising effect, a premature leakage of entrapped bioactive compounds might occur in the gut prior to intestinal absorption.
منابع مشابه
A Review of Vesicular and Polymeric Nano-systems in Olanzapine Drug Delivery
Olanzapine (2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno [2, 3-b][1, 5]benzodiazepine) is an antipsychotic drug with poor water-solubility that has a suitable affinity to some receptors. This benzodiazepine derivative is a new (atypical) antipsychotic drug and has a wide range of efficacy, especially in treatment of patients with negative psychiatric symptoms of schizophrenia. Olanzapine is ...
متن کاملEvaluation of Lipid-based Drug Delivery System (Phytosolve) on Oral Bioavailability of Dibudipine
Abstract The objective of present study was to evaluate pharmacokinetic parameters of dibudipine Phytosolve after oral administration in rats. The solubility test was carried out to select suitable oily solvent for dibudipine. Phytosolve formulation was prepared with a medium chain triglyceride (MCT) oil (20%), soybean phospholipids (5%) and a 70% fructose solution (75%). The effect of polyol c...
متن کاملEvaluation of Lipid-based Drug Delivery System (Phytosolve) on Oral Bioavailability of Dibudipine
Abstract The objective of present study was to evaluate pharmacokinetic parameters of dibudipine Phytosolve after oral administration in rats. The solubility test was carried out to select suitable oily solvent for dibudipine. Phytosolve formulation was prepared with a medium chain triglyceride (MCT) oil (20%), soybean phospholipids (5%) and a 70% fructose solution (75%). The effect of polyol c...
متن کاملFormulation of mefenamic acid loaded transfersomal gel by thin film hydration technique and hand shaking method
Objective(s): The aim of present study is to formulate mefenamic acid transdermal gel based on vesicular drug delivery approaches.Materials and Methods: For the preparation of mefenamic acid transdermal gel, transfersomes were selected as colloidal carriers. Transfersomes were prepared by hand shaking and thin film hydration techniques. The obtained transfersomes were characterized for vesicula...
متن کاملStorage Stability of Wheat Germ Oil Encapsulated within Nanostructured Lipid Carriers
The present study aimed to evaluate the effect of surfactant composition on the physical properties of nanostructured lipid carriers (NLCs) containing wheat germ oil (WGO) and to investigate the influence of both surfactant composition and pH on the oxidative stability of WGO encapsulated within the NLCs. The results showed that the smallest particle size (52.7 nm) was related to the NLC with t...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
دوره شماره
صفحات -
تاریخ انتشار 2016