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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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Mechanisms of Drug Absorption: Paracellular, Transcellular, and Vesicular Transport01:23

Mechanisms of Drug Absorption: Paracellular, Transcellular, and Vesicular Transport

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Drugs need to permeate cell membranes to reach their target sites after administration. Orally administered drugs must transcend intestinal epithelial membrane barriers to infiltrate the systemic circulation. Drugs with a molecular weight of less than 500 Daltons diffuse through gaps between neighboring cells, called paracellular pathways.
However, most drugs use the transcellular route, traversing directly through the cell membranes via two mechanisms: passive and active transport. Passive...
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Methods for Studying Drug Absorption: In vitro01:16

Methods for Studying Drug Absorption: In vitro

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In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
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Drug Delivery: Overview01:16

Drug Delivery: Overview

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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...
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Routes of Drug Administration: Enteral01:18

Routes of Drug Administration: Enteral

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Medications can be administered through the enteral route using liquids, capsules, or tablets.
Enteral administration involves drug administration via the mouth in two ways: orally or sublingually.
Unlike sublingually drugs, drugs that are taken orally pass through the gastrointestinal (GI) tract and get metabolized by the liver. Once metabolized, the drug is absorbed into the systemic circulation, reaching different body parts via the bloodstream. However, while passing through the stomach,...
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Routes of Drug Administration: Parenteral01:25

Routes of Drug Administration: Parenteral

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The administration of drugs via parenteral routes allows for direct drug introduction into the systemic circulation, resulting in high bioavailability because the medication bypasses the harsh conditions of the gastrointestinal tract and hepatic metabolism.
The intravenous route (IV) of drug administration can be further categorized into two types. The bolus injection administers the entire dose rapidly, while an intravenous infusion slowly delivers smaller doses steadily.
The IV route is often...
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Related Experiment Video

Updated: May 9, 2025

Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins
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Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins

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Enhancing Intracellular Uptake of Ivermectin through Liposomal Encapsulation.

Meryem Kocas1,2,3,4, Fumiyoshi Yamashita5,4, Tansel Comoglu6

  • 1Faculty of Pharmacy, Department of Pharmaceutical Technology, Selcuk University, Selçuklu, Konya, 42130, Turkey.

AAPS Pharmscitech
|May 2, 2025
PubMed
Summary
This summary is machine-generated.

Liposomal encapsulation significantly improves ivermectin (IVM) delivery by enhancing cellular uptake and reducing cytotoxicity. This formulation strategy shows promise for increasing the therapeutic effectiveness of IVM against various diseases.

Keywords:
Vero E6cellular uptakeenhancing cellular uptakeivermectinliposomes

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Using In Vitro Live-cell Imaging to Explore Chemotherapeutics Delivered by Lipid-based Nanoparticles
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Area of Science:

  • Pharmacology
  • Drug Delivery Systems
  • Nanotechnology

Background:

  • Ivermectin (IVM) is an antiparasitic drug with potential antiviral applications, but its poor water solubility limits bioavailability.
  • Liposomes are effective drug carriers, enhancing solubility, enabling targeted delivery, and controlling release kinetics for lipophilic drugs.

Purpose of the Study:

  • To develop and evaluate liposomal formulations of ivermectin (IVM) to improve its cellular uptake and reduce cytotoxicity.
  • To compare the in vitro cellular uptake and cytotoxicity of free IVM versus IVM-loaded liposomes in Vero E6 cells.

Main Methods:

  • Liposomal formulations of IVM were prepared using soyphosphatidylcholine, dioleylphosphatidylcholine, cholesterol, and diethylphosphate via the ethanol injection method.
  • Physicochemical properties of liposomes were previously characterized; this study focused on in vitro cellular uptake and cytotoxicity assays.
  • Vero E6 cells were used to assess the half-maximal cytotoxic concentrations (CC50) and cellular uptake percentages for free IVM and IVM-loaded liposomes.

Main Results:

  • Liposomal encapsulation significantly increased IVM cellular uptake, ranging from 13% to 60%, compared to only 2% for free IVM.
  • The half-maximal cytotoxic concentration (CC50) of IVM-loaded liposomes was substantially higher (>110 μM) than that of free IVM (10 μM), indicating reduced toxicity.
  • Liposomal formulation enhanced IVM's therapeutic index by improving uptake and decreasing cytotoxicity.

Conclusions:

  • Liposomal encapsulation is a viable strategy to overcome the limitations of ivermectin's poor solubility and bioavailability.
  • This approach enhances IVM's cellular delivery and reduces its inherent cytotoxicity, paving the way for improved therapeutic efficacy.
  • The developed liposomal IVM formulations represent a promising advancement for treating neglected tropical diseases and potentially viral infections.