Related Experiment Video
Updated: Jan 7, 2026
08:18
Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
1.5K
Comparative Study on Cannabidiol-Loaded Solubilizing Systems for Improvement of Oral Bioavailability: Liposome and
Hideyuki Sato1, Kenta Watanabe1, Ryuji Yagi2
1Laboratory of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan.
Biopharmaceutics & Drug Disposition
|December 27, 2025
Summary
Developing liposomal cannabidiol (LIP/CBD) significantly enhances its dissolution and oral bioavailability (BA) compared to crystalline CBD. This liposomal formulation offers a promising strategy for improving CBD
Area of Science:
- Pharmacology and Pharmaceutics
- Drug Delivery Systems
- Lipid-based Formulations
Background:
- Cannabidiol (CBD) exhibits poor physicochemical properties, including low solubility and dispersibility, limiting its oral bioavailability.
- First-pass metabolism further reduces the systemic exposure of orally administered CBD.
- Conventional solubilization systems, like cyclodextrin-based formulations (CD/CBD), offer some improvement but may not fully address CBD's limitations.
Purpose of the Study:
- To develop a liposomal cannabidiol (LIP/CBD) formulation to enhance CBD's physicochemical properties and oral bioavailability (BA).
- To compare the biopharmaceutical performance of LIP/CBD with crystalline CBD and a conventional cyclodextrin-based formulation (CD/CBD).
Main Methods:
- Liposomal cannabidiol (LIP/CBD) was prepared using the solvent injection method.
- Physicochemical characterization included particle size, zeta potential, and dissolution studies at simulated intestinal pH.
- Pharmacokinetic evaluation involved oral administration in vivo to assess systemic exposure and Tmax.
Main Results:
- LIP/CBD exhibited uniform spherical liposomes (~120 nm, PDI 0.13, zeta potential -68 mV).
- LIP/CBD demonstrated an 8-fold increase in CBD dissolution compared to crystalline CBD.
- Oral administration of LIP/CBD resulted in a 22-fold higher systemic exposure than crystalline CBD, significantly outperforming CD/CBD (5.3-fold increase).
Conclusions:
- Liposomal encapsulation is a viable strategy to overcome CBD's poor solubility and enhance its dissolution and oral absorption.
- LIP/CBD offers superior biopharmaceutical advantages over crystalline CBD and conventional cyclodextrin formulations.
- The enhanced lymphatic absorption potentially contributed by lipidic components may explain the prolonged Tmax of LIP/CBD.
Related Concept Videos
01:16Bioavailability Enhancement: Drug Solubility Enhancement
197
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...
197
01:27Bioavailability Enhancement: Drug Permeability Enhancement
174
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...
174
01:22Bioavailability Enhancement: Determination and Conceptual Approaches in Overcoming Bioavailability Problems
150
Body:Bioavailability is a critical pharmacological concept that measures the extent and rate at which an active drug ingredient or therapeutic moiety enters the systemic circulation, remaining unchanged. It's a pivotal factor in determining a drug's efficacy and safety.The Biopharmaceutics Classification System (BCS) plays an essential role in drug development by categorizing drugs into four classes based on their solubility and permeability. This classification aids in understanding drug...
150
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
180
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...
180
01:27Factors Influencing Drug Absorption: Drug Dissolution
1.1K
The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
1.1K
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
477
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...
477