Overview of Extensively Employed Polymeric Carriers in Solid Dispersion Technology
Athira R Nair1, Yarlagadda Dani Lakshman1, Vullendula Sai Krishna Anand1
1Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, 576 104, India.
AAPS Pharmscitech
|November 8, 2020
Summary
Solid dispersion technology enhances drug efficacy for poorly soluble compounds. This review analyzes key polymeric carriers like PVP and PEG, aiding formulators in selecting optimal materials for improved dissolution and stability.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Solid dispersion is a key technology for enhancing the bioavailability of poorly soluble drugs (BCS class-II/IV APIs).
- Numerous polymeric carriers with diverse properties are available for formulating solid dispersions.
- Over 5000 scientific papers highlight the significance of solid dispersion technology since the 1960s.
Purpose of the Study:
- To review the properties of extensively used polymeric carriers in solid dispersion technology.
- To analyze literature trends in preparation techniques, dissolution, and stability improvement.
- To guide formulators in selecting appropriate polymeric carriers for solid dispersions.
Main Methods:
- Literature analysis of polymeric carriers including PVP, Copovidone, PEG, HPMC, HPMCAS, and Soluplus®.
- Data extraction from the Scopus® database focusing on preparation, dissolution, and stability.
- Evaluation of polymer properties relevant to solid dispersion formulation.
Main Results:
- The choice of polymeric carrier significantly impacts the stability and dissolution enhancement of solid dispersions.
- Analysis of literature trends reveals key preparation methods and their effects on drug performance.
- Specific polymers like PVP, PEG, and Soluplus® show distinct advantages depending on application.
Conclusions:
- Formulator's choice of polymeric carrier is critical for successful solid dispersion development.
- Further research is needed to evaluate polymer performance under dynamic pH shift conditions.
- Development of a regulatory framework for solid dispersion characterization is essential.
More Related Videos
Related Concept Videos
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
290
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...
290
01:27Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
83
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,...
83
01:05Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
103
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...
103
01:16Drug Delivery: Overview
594
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...
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
594
01:16Bioavailability Enhancement: Drug Solubility Enhancement
114
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...
114
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
539
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...
539