Related Experiment Video
Updated: May 5, 2026
07:53
Encapsulation of Cancer Therapeutic Agent Dacarbazine Using Nanostructured Lipid Carrier
Published on: April 26, 2016
10.2K
Liposomal Encapsulation of Camptothecin/Carboxymethyl-β-Cyclodextrin Complexes: Stability, Solubility and
Fernando Mesías-Recamán1,2, Alba Durán-Moreno3, Thais Carmona3,4
1Department of Chemical Engineering, University of Salamanca, Plaza Caidos S-N, 37008 Salamanca, Spain.
International Journal of Molecular Sciences
|May 4, 2026
Summary
Carboxymethyl-beta-cyclodextrin (cmβCD) enhances anticancer drug camptothecin (CPT) solubility and liposomal loading. This improves CPT delivery and efficacy, offering a promising strategy for cancer therapy.
Area of Science:
- Pharmaceutical Chemistry
- Drug Delivery Systems
- Nanotechnology
Background:
- Camptothecin (CPT) exhibits poor aqueous solubility and bloodstream instability, limiting its clinical use.
- Effective drug delivery strategies are needed to enhance CPT bioavailability and therapeutic efficacy.
Purpose of the Study:
- To investigate the complexation of CPT with carboxymethyl-beta-cyclodextrin (cmβCD) to improve its solubility and facilitate liposomal drug delivery.
- To evaluate the impact of pH on CPT-cmβCD complex stability and binding interactions.
Main Methods:
- Fluorescence spectroscopy and molecular modeling were used to characterize CPT-cmβCD inclusion complexes.
- Solubility, liposomal loading, drug release kinetics, and in vitro cytotoxicity assays were performed.
- A cationic amino-beta-cyclodextrin (amβCD) was used as a control to elucidate binding mechanisms.
Main Results:
- Complexation with cmβCD enhanced CPT solubility up to 11-fold.
- Liposomal loading of CPT was increased by 385-fold using the cmβCD system.
- CPT-loaded liposomes showed significant cytotoxicity against cancer cell lines, with stability at physiological pH and release in acidic conditions.
Conclusions:
- cmβCD complexation effectively improves CPT solubility and liposomal loading capacity.
- This approach offers a viable strategy for enhancing CPT delivery and anticancer activity.
- The pH-dependent stability and release profile of liposomes are crucial for targeted drug delivery.
Related Concept Videos
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
332
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...
332
01:27Bioavailability Enhancement: Drug Permeability Enhancement
352
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 secretion,...
352
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
733
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...
733
01:16Bioavailability Enhancement: Drug Solubility Enhancement
499
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...
499
01:24Site-Targeted Drug Delivery Systems: Polymeric Carriers
160
Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
160
01:21Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
4.4K
Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
4.4K