Labrasol-Enriched Nanoliposomal Formulation: Novel Approach to Improve Oral Absorption of Water-Insoluble Drug, Carvedilol

AAPS PharmSciTech
Samaneh GhassemiSimin Dadashzadeh

Abstract

The purpose of the current study was to develop a novel liposomal formulation to improve the oral bioavailability of carvedilol, a Biopharmaceutics Classification System class II with poor aqueous solubility and extensive presystemic metabolism. Conventional and various surfactant-enriched carvedilol-loaded liposomes were prepared by thin film hydration technique and physicochemical properties of liposomes (including size, encapsulation efficiency, release behavior, and morphology) were evaluated. To assess the oral bioavailability, in vivo studies were carried out in eight groups of male Wistar rats (n = 6) and the drug plasma concentration was determined. Conventional and surfactant containing liposomes showed average particle size of 76-104 nm with a narrow size distribution, high encapsulation efficiency (80%≤) and a sustained release profile in simulated intestinal fluid. Compared to the suspension, conventional and Labrasol containing liposomes significantly improved the oral bioavailability and peak plasma concentration of carvedilol. Biocompatibility studies (cell cytotoxicity and histopathological analyses) showed that the enhancing effect might be achieved without any apparent toxicity in the intestine. Decreased oral...Continue Reading

References

May 1, 1994·Clinical Pharmacokinetics·T Morgan
Oct 23, 2002·Circulation·Milton PackerUNKNOWN Carvedilol Prospective Randomized Cumulative Survival (COPERNICUS) Study Group
May 8, 2004·International Journal of Pharmaceutics·Y V Rama PrasadKanji Takada
Oct 7, 2004·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Maria E F da Silva, Nilce C Meirelles
Mar 31, 2005·Journal of Colloid and Interface Science·Xuemei LiangK Y Simon Ng
Jun 14, 2005·British Journal of Pharmacology·Joost BartN Harry Hendrikse
Jun 22, 2005·Biopharmaceutics & Drug Disposition·Anooshirvan ShayeganpourDion R Brocks
May 5, 2006·Fundamental & Clinical Pharmacology·Iouri BachmakovMartin F Fromm
Mar 3, 2007·Nature Reviews. Drug Discovery·Christopher J H PorterWilliam N Charman
Aug 5, 2008·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Marianne L LindAnette Müllertz
Jan 16, 2010·Expert Opinion on Drug Metabolism & Toxicology·Subhashis ChakrabortySanjay Singh
Feb 24, 2010·Computer Methods and Programs in Biomedicine·Yong ZhangShaofei Xie
Apr 23, 2010·Pharmaceutical Research·Gert FrickerChristel Müller-Goymann
Jan 12, 2011·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Anne ChristiansenWerner Weitschies
Feb 10, 2011·Journal of Drug Targeting·Yaw-Bin HuangJia-You Fang
Mar 3, 2011·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Javed IqbalAndreas Bernkop-Schnürch
Jun 30, 2011·Advanced Drug Delivery Reviews·Shuang CaiM Laird Forrest
Mar 1, 2012·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Mengmeng NiuWei Wu
Sep 7, 2012·Drug Discovery Today·Silvia MazzaferroGilles Ponchel
Oct 31, 2012·Journal of Pharmacy & Pharmaceutical Sciences : a Publication of the Canadian Society for Pharmaceutical Sciences, Société Canadienne Des Sciences Pharmaceutiques·Elmira BajelanSimin Dadashzadeh
Mar 15, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Yuanyuan GuoZhiping Zhang
Apr 5, 2014·The Journal of Pharmacy and Pharmacology·Yue ZhouJin Deng
May 24, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Shasha RaoClive A Prestidge
Sep 16, 2014·Artificial Cells, Nanomedicine, and Biotechnology·Hadis DaraeeAbolfazl Akbarzadeh
Sep 18, 2014·Recent Patents on Anti-cancer Drug Discovery·Mohd A AlamRaisuddin Ali
Sep 23, 2014·Artificial Cells, Nanomedicine, and Biotechnology·Supandeep Singh HallanBhuvaneshwar Vaidya
Sep 23, 2014·PloS One·Adrien JacquotElmira Arab-Tehrany
Dec 30, 2014·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Yating ShaoHyo-Kyung Han
Feb 11, 2015·Clinical Pharmacokinetics·Kamla Pathak, Smita Raghuvanshi
May 20, 2015·Colloids and Surfaces. B, Biointerfaces·Yaowaporn SangsenRuedeekorn Wiwattanapatapee
Dec 23, 2015·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Kesinee NetsomboonAndreas Bernkop-Schnürch
Jun 29, 2016·Expert Opinion on Drug Delivery·Lungile Nomcebo ThwalaNoémi Stefania Csaba
Oct 6, 2016·Journal of Microencapsulation·Jagruti Desai, Hetal Thakkar

❮ Previous
Next ❯

Citations

Jan 24, 2019·AAPS PharmSciTech·Nikhar VishwakarmaSuresh P Vyas
Dec 2, 2020·Pharmaceutics·Line SéguyAurélie Malzert-Fréon
Mar 1, 2020·Journal of Controlled Release : Official Journal of the Controlled Release Society·Delaram BabadiAzadeh Haeri
Nov 14, 2020·Drug Development and Industrial Pharmacy·Nayera NasserOmaima A Sammour

❮ Previous
Next ❯

Methods Mentioned

BETA
atomic force microscopy
scraping
protein assay
ELISA
AFM

Software Mentioned

GraphPad Prism
GraphPad
PKSolver

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
Hyo-Kyung HanDong Hoon Ha
© 2022 Meta ULC. All rights reserved