Abstract
Background: In 1995, the Biopharmaceutics Classification System (BCS) was proposed by Amidon and colleagues as a tool that considers two important parameters regarding drugs: solubility and permeability. Since then, several methods for solubility and permeability studies have been developed for drug delivery and absorption prediction. In recent years, permeability has gained a great highlight and the interaction between a molecule and a biological membrane is not enough to predict the in vivo behavior of a compound.
Method: Thus, different methods for permeability assessment are currently used for mechanistic studies including involvement of carriers and several transport pathways. Furthermore, the investigation regarding metabolism has been a focus in recent researches. Based on this idea, Wu and Benet proposed a new tool called Biopharmaceutics Drug Disposition Classification System (BDDCS), where drugs are classified into four classes considering their solubility and metabolism. Results: Among several methods for permeability studies, the in situ intestinal perfusion is considered the closest to in vivo conditions due advantages as intact blood supply and innervation. Conclusion: This review presents the in situ intestinal perfusion model and its application for permeability/ transport studies of drugs and intestinal metabolism. Also, this paper discusses about how the in situ perfusion studies can be used for classification of drugs and the future perspectives for in vivo absorption prediction.Keywords: BCS, BDDCS, in situ perfusion, intestinal metabolism, permeability, transport.
Mini-Reviews in Medicinal Chemistry
Title:In Situ Intestinal Perfusion in Rodents: Future Perspectives for Application on Absorption Studies and Classification of Drugs
Volume: 17 Issue: 9
Author(s): Thaisa Marinho Dezani, Andre Bersani Dezani, Monica Maria Coquemala de Silva and Cristina Helena dos Reis Serra*
Affiliation:
- Department of Pharmacy, Faculty of Pharmaceutical Sciences of the University of Sao Paulo - Avenida Professor Lineu Prestes, 580, Bl. 13, 05508-900, Sao Paulo, SP,0
Keywords: BCS, BDDCS, in situ perfusion, intestinal metabolism, permeability, transport.
Abstract: Background: In 1995, the Biopharmaceutics Classification System (BCS) was proposed by Amidon and colleagues as a tool that considers two important parameters regarding drugs: solubility and permeability. Since then, several methods for solubility and permeability studies have been developed for drug delivery and absorption prediction. In recent years, permeability has gained a great highlight and the interaction between a molecule and a biological membrane is not enough to predict the in vivo behavior of a compound.
Method: Thus, different methods for permeability assessment are currently used for mechanistic studies including involvement of carriers and several transport pathways. Furthermore, the investigation regarding metabolism has been a focus in recent researches. Based on this idea, Wu and Benet proposed a new tool called Biopharmaceutics Drug Disposition Classification System (BDDCS), where drugs are classified into four classes considering their solubility and metabolism. Results: Among several methods for permeability studies, the in situ intestinal perfusion is considered the closest to in vivo conditions due advantages as intact blood supply and innervation. Conclusion: This review presents the in situ intestinal perfusion model and its application for permeability/ transport studies of drugs and intestinal metabolism. Also, this paper discusses about how the in situ perfusion studies can be used for classification of drugs and the future perspectives for in vivo absorption prediction.Export Options
About this article
Cite this article as:
Dezani Marinho Thaisa, Dezani Bersani Andre, de Silva Maria Coquemala Monica and dos Reis Serra Helena Cristina*, In Situ Intestinal Perfusion in Rodents: Future Perspectives for Application on Absorption Studies and Classification of Drugs, Mini-Reviews in Medicinal Chemistry 2017; 17 (9) . https://dx.doi.org/10.2174/1389557516666160921145613
DOI https://dx.doi.org/10.2174/1389557516666160921145613 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
RNA Interference and Potential Applications
Current Topics in Medicinal Chemistry Recent Studies and Biological Aspects of Substantial Indole Derivatives with Anti-cancer Activity
Current Organic Chemistry Dihydrofolate Reductase Gene Variations in Susceptibility to Disease and Treatment Outcomes
Current Genomics Proteomic Approaches for the Study of Transgelins as Tumor-associated Proteins and Potential Biomarkers
Current Proteomics The Cellular Pharmacokinetics of HIV Protease Inhibitors: Current Knowledge and Future Perspectives
Current Drug Metabolism Drug Design Targeting the CXCR4/CXCR7/CXCL12 Pathway
Current Topics in Medicinal Chemistry MicroRNAs Patents: The Road From Bench to Bedsides for Cancer Treatment
Recent Patents on DNA & Gene Sequences Topoisomerase 1B as a Target Against Leishmaniasis
Mini-Reviews in Medicinal Chemistry Targeted Therapy Towards Cancer-A Perspective
Anti-Cancer Agents in Medicinal Chemistry Trans-Platinum Complexes in Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Lipids and Their Derivatives: By-Products Used as Essential Building Blocks for Modern Drug Delivery Systems
Current Drug Targets Pathological and Therapeutic Aspects of Long Noncoding RNAs in Osteosarcoma
Anti-Cancer Agents in Medicinal Chemistry TargetMM: Accurate Missense Mutation Prediction by Utilizing Local and Global Sequence Information with Classifier Ensemble
Combinatorial Chemistry & High Throughput Screening Mechanistic Insights into the Antileukemic Activity of Hyperforin
Current Cancer Drug Targets Patent Selections:
Recent Patents on Drug Delivery & Formulation Nab-Paclitaxel in Metastatic Breast Cancer: Defining the Best Patient Profile
Current Cancer Drug Targets The Role of Lymphotoxin Receptor Signaling in Diseases
Current Molecular Medicine Patent Selections
Recent Patents on Anti-Infective Drug Discovery The Akt Pathway: Molecular Targets for Anti-Cancer Drug Development
Current Cancer Drug Targets Regulation of Autophagy in Oxygen-Dependent Cellular Stress
Current Pharmaceutical Design