Related Experiment Video

Updated: Dec 24, 2025

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers
18:57

Models and Methods to Evaluate Transport of Drug Delivery Systems Across Cellular Barriers

Published on: October 17, 2013

47.1K

Intestinal OCTN2- and MCT1-targeted drug delivery to improve oral bioavailability

Gang Wang1, Lichun Zhao1,2, Qikun Jiang3

  • 1Zhuang Yao Medicine Center of Engineering and Technology, Guang Xi University of Chinese Medicine, Nanning 530200, China.

Asian Journal of Pharmaceutical Sciences
|April 8, 2020
PubMed

Insights

Targeting intestinal transporters like carnitine/organic cation transporter 2 (OCTN2) and mono-carboxylate transporter 1 (MCT1) enhances oral drug delivery. Prodrugs and nanoparticles show promise for improving the absorption of various medications.

Area of Science:

  • Pharmacology
  • Drug Delivery
  • Biochemistry

Background:

  • Intestinal drug transporters are crucial for nutrient and drug absorption.
  • Carnitine/organic cation transporter 2 (OCTN2) and mono-carboxylate transporter 1 (MCT1) have high transport capacities and complementary distributions.
  • These transporters are key targets for enhancing oral drug delivery.

Purpose of the Study:

  • To review recent advancements in oral drug delivery strategies targeting OCTN2 and MCT1.
  • To discuss the development of prodrugs and nanoparticles for transporter-mediated drug absorption.
  • To explore the potential of dual transporter-targeting approaches.

Main Methods:

  • Review of existing literature on OCTN2 and MCT1.
  • Analysis of prodrug and nanoparticle design for transporter targeting.
  • Examination of clinical applications for anti-inflammatory, antiepileptic, and anticancer drugs.

Main Results:

  • Detailed information on the structure, function, and substrates of OCTN2 and MCT1.
  • Demonstrated improvements in oral absorption of various drugs using transporter-targeted strategies.
  • Evidence supporting the efficacy of prodrugs and nanoparticles in enhancing oral bioavailability.

Conclusions:

  • OCTN2 and MCT1 are promising targets for improving oral drug delivery.
  • Prodrugs and nanoparticles offer effective strategies for transporter-mediated drug absorption.
  • Dual targeting of OCTN2 and MCT1 presents a potential future direction for enhanced oral drug delivery.
Keywords:
Carnitine/organic cation transporter 2 (OCTN2)Monocarboxylate transporter protein 1 (MCT1)NanoparticleProdrugTransporter-targeting

More Related Videos

Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier10:16

Targeted Plasma Membrane Delivery of a Hydrophobic Cargo Encapsulated in a Liquid Crystal Nanoparticle Carrier

Published on: February 8, 2017

7.9K
An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment08:59

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment

Published on: December 3, 2020

8.4K

Related Concept Videos

Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
138
Drug Delivery: Enteral Route01:18

Drug Delivery: Enteral Route

The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
1.4K
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

Bioavailability Enhancement: Drug Stability Enhancement and GI Retention

Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
143
Carrier-Mediated Transport01:06

Carrier-Mediated Transport

Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
910
Bioavailability Enhancement: Drug Solubility Enhancement01:16

Bioavailability Enhancement: Drug Solubility Enhancement

Body:Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
157
Drug Delivery: Overview01:16

Drug Delivery: Overview

The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
652