Formulation, in-vitro evaluation and optimization of valsartan nano-lipid complex by Box-Behnken design. 2023

- Magdy I Mohamed, and - Hanaa A Mahmoud, and - Amir I Mohamed, and - Nesrin M Nabil, and - Mohamed A Kasssem, and - Yousef A Elsherif
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

The antihypertensive drug valsartan, has an imperfect bioavailability due to its low solubility, permeability and excessive first pass hepatic metabolism. So, the goal of this article is to improve the physicochemical properties of valsartan to increase its bioavailability. In order to achieve this goal, valsartan- phospholipid complexsomes (VAL-PLC) were developed by the technique of solvent evaporation using Box-Behnken experimental design to optimize variables in the production process. The box- Behnken design revealed that the formula F3 prepared using 60% lipid percentage at 600C reaction temperature for 2h reaction time offered the optimum conditions for VAL-PLC preparation where the percent drug content reached 92.24%, average particle diameter was 189.17nm and polydispersity index was 0.289. Drug release experiment indicated that the dissolution of both raw valsartan and its commercial dosage form was dependent upon pH where it was extremely low at pH 1.2 and low in distilled water and it had a high dissolution at pH 6.8. On the contrary, the optimized VAL-PLC formula showed a high and pH-independent dissolution rate whatever the type of dissolution medium was. Therefore, it was concluded that valsartan-complexsomes may be considered as an encouraging approach for improving physicochemical properties and increasing bioavailability of valsartan.

UI MeSH Term Description Entries
D010539 Permeability Property of membranes and other structures to permit passage of light, heat, gases, liquids, metabolites, and mineral ions. Permeabilities
D010743 Phospholipids Lipids containing one or more phosphate groups, particularly those derived from either glycerol (phosphoglycerides see GLYCEROPHOSPHOLIPIDS) or sphingosine (SPHINGOLIPIDS). They are polar lipids that are of great importance for the structure and function of cell membranes and are the most abundant of membrane lipids, although not stored in large amounts in the system. Phosphatides,Phospholipid
D000068756 Valsartan A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION. CGP 48933,Diovan,Kalpress,Miten,N-valeryl-N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)valine,Nisis,Provas,Tareg,Vals,48933, CGP
D000959 Antihypertensive Agents Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. Anti-Hypertensive,Anti-Hypertensive Agent,Anti-Hypertensive Drug,Antihypertensive,Antihypertensive Agent,Antihypertensive Drug,Anti-Hypertensive Agents,Anti-Hypertensive Drugs,Anti-Hypertensives,Antihypertensive Drugs,Antihypertensives,Agent, Anti-Hypertensive,Agent, Antihypertensive,Agents, Anti-Hypertensive,Agents, Antihypertensive,Anti Hypertensive,Anti Hypertensive Agent,Anti Hypertensive Agents,Anti Hypertensive Drug,Anti Hypertensive Drugs,Anti Hypertensives,Drug, Anti-Hypertensive,Drug, Antihypertensive,Drugs, Anti-Hypertensive,Drugs, Antihypertensive
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D065546 Drug Liberation Release of drugs from DOSAGE FORMS into solution. Drug Dissolution,Drug Release,Dissolution, Drug,Liberation, Drug,Release, Drug

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