Related Experiment Video
Updated: Jul 2, 2026
07:32
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Development and characterization of bicalutamide-poloxamer F68 solid dispersion systems
P P Sancheti1, V M Vyas, M Shah
1Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad, Maharashtra, India.
Die Pharmazie
|September 6, 2008
Summary
This study enhanced bicalutamide dissolution using solid dispersions with poloxamer F68. The optimal 1:1 ratio significantly improved drug release, overcoming poor water solubility.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Bicalutamide is a poorly water-soluble drug.
- Enhancing dissolution rate is crucial for improving bioavailability.
Purpose of the Study:
- To improve the dissolution rate of bicalutamide.
- To prepare and evaluate bicalutamide-poloxamer F68 solid dispersion systems.
Main Methods:
- Solid dispersions prepared using the melting method with poloxamer F68 at 1:1, 1:3, and 1:5 ratios.
- Drug-polymer interactions analyzed by TLC, FTIR, and powder X-ray diffraction (XRD).
- Dissolution rates evaluated for pure bicalutamide and its solid dispersions.
Main Results:
- Powder XRD confirmed a significant decrease in bicalutamide crystallinity within the binary systems.
- All bicalutamide solid dispersions exhibited significantly faster dissolution compared to the pure drug (p < 0.001).
- The 1:1 bicalutamide:poloxamer F68 ratio demonstrated excellent dissolution enhancement (DP30: 99.98% ± 3.9).
- Higher poloxamer F68 ratios (1:3, 1:5) retarded drug release, potentially due to gelling properties.
Conclusions:
- Solid dispersion technique effectively enhances bicalutamide dissolution rate.
- The 1:1 bicalutamide:poloxamer F68 solid dispersion is optimal for improving drug release.
- Poloxamer F68 concentration influences drug release kinetics, with higher concentrations potentially hindering it.
Related Concept Videos
01:27Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
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...
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
01:16Bioavailability Enhancement: Drug Solubility Enhancement
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...
01:24Site-Targeted Drug Delivery Systems: Polymeric Carriers
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...