Enhancing solubility and stability of poorly soluble drugs.
Journal name: World Journal of Pharmaceutical Research
Original article title: Synergistic effect of solid dispersion and inclusion complex in enhancing the solubility and stability of poorly soluble drugs
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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Kofi Oti Boakye-Yiadom, Samuel Kesse, Mensura Sied Filli, Md. Aquib, Faisal Raza, Reyaj Mikrani and Wang Bo
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Synergistic effect of solid dispersion and inclusion complex in enhancing the solubility and stability of poorly soluble drugs
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr201817-13387
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
1. Introduction
The review paper discusses the challenges associated with the poor aqueous solubility of many pharmaceutical compounds, particularly those that are weakly acidic or basic. Various techniques exist to enhance the solubility and bioavailability of these poorly soluble drugs, including micronization, pH adjustment, and complexation methods. Among these techniques, inclusion complexation and solid dispersion stand out as effective methods for improving drug solubility. The review emphasizes the synergistic effect that can result from combining both techniques, ultimately leading to enhanced wettability, smaller particle size, and improved bioavailability.
2. The Role of Cyclodextrins in Drug Solubility
Cyclodextrins (CDs), discovered by French scientist Villiers and further studied by Schardinger, have gained considerable attention for their ability to form inclusion complexes with poorly soluble drugs. The unique structure of cyclodextrins, with a hydrophobic cavity that can encapsulate drug molecules, allows for improved water solubility. This complex formation alters the physical and chemical properties of the drug, enhancing both its solubility and bioavailability. However, it is important to monitor the possible toxicity of certain types of cyclodextrins, particularly β-cyclodextrin, when used for parenteral purposes, as it may induce nephrotoxicity.
3. Solid Dispersions as a Strategy for Solubility Enhancement
Solid dispersions (SDs) have been employed since the 1960s as a formulation strategy to improve the solubility of poorly soluble drugs. These dispersions can further be categorized into eutectic mixtures, solid solutions, and microfine crystalline dispersions depending on the method of incorporation of the drug within a hydrophilic carrier. Techniques such as solvent evaporation, hot-melt extrusion, and lyophilization are utilized to create solid dispersions, which have shown to significantly enhance the dissolution rate and solubility of various pharmaceutical compounds. Characterization methods are crucial to ensuring the effectiveness of these formulations and their stability over time.
4. Synergistic Effects of Combined Techniques
The review highlights the advantages of combining solid dispersion and inclusion complexation to maximize the solubility and bioavailability of drugs. Studies demonstrated that this combination leads to a notable decrease in particle size and an increase in amorphous drug forms, ultimately resulting in better drug performance. For example, the use of hydroxypropyl-β-cyclodextrin alongside polymers like Poloxamer 188 and Polyvinylpyrrolidone K-30 has been shown to significantly enhance the solubility and stability of carvedilol. However, the stability of these combined systems may be compromised by factors such as aging and environmental conditions, necessitating ongoing research in combinatorial approaches.
5. Conclusion
In conclusion, the poor bioavailability of drugs remains a significant hurdle in pharmaceutical formulation, which can be addressed through effective solubility-enhancing techniques like inclusion complexation and solid dispersion. Both methods offer unique benefits, but their combination can yield superior results. Future research should focus on exploring additional combinatorial strategies to further improve the solubility and stability of drugs, thus expanding the therapeutic potential of poorly soluble compounds. The authors acknowledge the contributions of various researchers and the support from China Pharmaceutical University, emphasizing the collaborative effort required to advance this field.
FAQ section (important questions/answers):
What are the main challenges with poorly soluble drugs?
Poorly soluble drugs face bioavailability issues, limiting their absorption and effectiveness. Techniques like solid dispersion and inclusion complexation can improve solubility and stability, helping these drugs reach their target sites in the body.
How do cyclodextrins enhance drug solubility?
Cyclodextrins form inclusion complexes with poorly soluble drugs, increasing their water solubility. The structure of cyclodextrins includes hydrophobic interiors that can host drug molecules, significantly improving their solubility and stability in pharmaceutical formulations.
What techniques improve solubility of poorly soluble drugs?
Techniques include micronization, pH adjustment, complexation, solid dispersion, and hydrotrophy. These methods help to enhance solubility, dissolution rates, and ultimately improve bioavailability for poorly soluble medications.
What are solid dispersions in drug formulation?
Solid dispersions are mixtures of hydrophobic drugs in hydrophilic carriers, improving solubility. They can be categorized into eutectic mixtures, solid solutions, and microfine crystalline dispersions to enhance drug performance.
What advantages do combination techniques offer?
Combination techniques of solid dispersion and inclusion complexation offer synergistic effects, improving the solubility and bioavailability of drugs. This strategy results in increased wettability, decreased particle size, and higher porosity.
What limitations exist with solubility enhancement techniques?
Limitations include challenges with preparation methods, reproducibility, physical and chemical stability, and scaling up manufacturing processes. Aging and environmental factors can also affect the stability of drug formulations.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Enhancing solubility and stability of poorly soluble drugs.”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.
1) Drug:
The term 'drug' refers to any substance used in the diagnosis, cure, treatment, or prevention of disease. In this context, poorly soluble drugs present a significant challenge in formulating effective medications, requiring novel techniques like solid dispersion and cyclodextrin complexation to enhance bioavailability and therapeutic efficacy.
2) Cina:
China is home to numerous pharmaceutical research institutions, including the China Pharmaceutical University. The country plays a pivotal role in the development of novel drug formulations aimed at improving drug solubility and stability, particularly for poorly soluble compounds through innovative techniques embraced by researchers in the region.
3) Pur:
The word 'poor' in this context is used to characterize the low solubility of certain drugs that adversely affect their bioavailability. The challenges of formulating these drugs necessitate various enhancement techniques, as their inefficacy can represent a significant therapeutic barrier impacting patient treatment outcomes.
4) Water:
Water is a critical solvent in pharmaceutical formulations, affecting the solubility of drugs. The solubility of poorly soluble compounds in water is crucial as it directly correlates with drug absorption in the gastrointestinal tract, influencing the overall bioavailability and therapeutic impact of medications.
5) Activity:
Activity refers to the pharmacological effects of drugs, including their therapeutic efficacy. The document focuses on enhancing the activity of poorly soluble drugs through innovative solubility enhancement techniques, ensuring that the active drug can effectively reach its target site and elicit the desired pharmacological response.
6) Table:
In the context of the article, 'table' could refer to the organized presentation of data, such as the tables describing solubility classifications or characterization methods. This format helps summarize important information, making it accessible for comparison and aiding in the understanding of drug formulations.
7) Surface:
Surface properties are important in the context of drug solubility and dispersion. The interaction of drug particles with solvents is heavily influenced by surface area, which can be optimized through techniques like solid dispersion to improve wettability, enhancing the dissolution rate and bioavailability of poorly soluble drugs.
8) Powder:
Powder is a common form of pharmaceutical formulation, particularly for solid drugs. The ability to manipulate and process powders into formulations like solid dispersions is crucial for improving the solubility and stability of poorly soluble drugs, enabling better absorption and therapeutic outcomes for patients.
9) Composite:
Composite refers to a material made from two or more constituent materials with significantly different physical or chemical properties. In pharmaceutical research, composites are often used to improve drug formulations by combining different substances that can enhance solubility, stability, and bioavailability, creating synergistic effects.
10) Medicine:
Medicine refers to the field focused on the diagnosis, treatment, and prevention of illness and injury. This word is integral to understanding the context of drug formulation and the importance of enhancing the solubility of poorly soluble drugs to ensure effective treatment and patient care.
11) Nature:
Nature refers to the inherent characteristics of substances, including their chemical and physical properties. In the context of drug formulation, understanding the nature of poorly soluble drugs allows researchers to devise effective strategies for enhancing solubility, stability, and bioavailability, ultimately improving therapeutic efficacy.
12) Animal:
Animal studies are crucial in preclinical research to assess the safety and efficacy of new drugs before human trials. This plays a critical role in understanding pharmacokinetics and pharmacodynamics, as well as validating formulations aimed at enhancing drug solubility for therapeutic applications in humans.
13) Sugar:
Sugar in this context refers to carbohydrate compounds often used as excipients in drug formulations. Certain sugars can serve as solid dispersion carriers, enhancing the solubility and bioavailability of poorly soluble drugs, thus helping to overcome formulation challenges faced in pharmaceutical development.
14) Field:
Field pertains to the area of expertise or study, in this case, pharmaceutical sciences. Continuous research in this field is essential for innovations in drug formulation technologies aimed at improving the solubility and stability of poorly soluble drugs, addressing crucial challenges in medication efficacy.
15) Food:
Food can be linked to the nutritional aspects of pharmaceuticals when taken orally. The presence of food can influence drug absorption and bioavailability, demanding research into formulation techniques that ensure therapeutic effectiveness, irrespective of dietary conditions while considering their solubility and stability.
16) Pharmacological:
Pharmacological relates to the effects, mechanisms, and actions of drugs in the body. The relevance lies in enhancing our understanding of how improved drug solubility techniques can impact the pharmacological activity of drugs, ultimately leading to more effective treatment options for patients.
17) Irritation:
Irritation pertains to the uncomfortable sensations that certain drugs may cause. The formulation strategies discussed aim to minimize irritation by enhancing drug solubility, thereby improving tolerability and patient adherence to medication regimens, which is vital for effective therapeutic outcomes.
18) Science (Scientific):
Scientific denotes the rigorous exploration and investigation methods applied to research. In the realm of pharmaceuticals, a scientific approach to solubility enhancement techniques is crucial for developing new drug formulations that effectively address the challenges associated with poorly soluble drugs, impacting patient care positively.
19) Education:
Education emphasizes the importance of knowledge dissemination in the field of pharmacology. Increased understanding of solubility techniques and drug formulation strategies is vital for training future professionals who can innovate in the pharmaceutical field and improve therapeutic outcomes for patients.
20) Yuvaraja (Yuvan-rajan, Yuvan-raja):
Yuvaraja likely refers to a researcher or author whose contributions to pharmaceutical science have aided in the exploration of techniques for improving drug solubility, emphasizing the importance of collaboration and authorship in advancing scientific knowledge and practices in the field.
21) Toxicity:
Toxicity refers to the adverse effects that drugs can have on biological systems. Understanding the toxicity profiles of formulation components, such as cyclodextrins, is essential for developing safe pharmaceutical applications, especially in the context of enhancing solubility while ensuring patient safety.
22) Heating:
Heating is a technique sometimes used in the preparation of solid dispersions to modify the physical state of drugs or carriers. It can facilitate better mixing and dispersion processes, contributing to improved solubility and dissolution rates of poorly soluble drugs in pharmaceutical formulations.
23) Mohana:
Mohana is likely another researcher or author noted for conducting studies on drug solubility and formulation strategies. The reference highlights the collaborative nature of scientific research, showcasing individuals contributing to advancing knowledge in improving the solubility of poorly soluble drugs.
24) Purity:
Purity refers to the absence of contaminants in a drug formulation. High purity levels in pharmaceutical compounds are essential for ensuring safety and efficacy, particularly when employing techniques like solid dispersion, which can alter drug characteristics and impact the therapeutic application.
25) Reason:
Reason signifies the logical basis for utilizing various solubility enhancement techniques. The challenge of poor bioavailability of drugs necessitates the employment of strategies such as solid dispersions and inclusion complexes, thereby underscoring the rationale behind their development in pharmaceutical sciences.
26) Blood:
Blood is the body's primary transport medium for nutrients and medications. Understanding the interaction between drug formulations and blood circulation is critical for assessing bioavailability and therapeutic response, particularly for poorly soluble drugs that require enhancement techniques to ensure effective systemic absorption.
27) Hand:
Hand indicates the practical aspect of pharmaceutical formulation. It emphasizes the skills and techniques required to manipulate and combine various agents in creating effective drug products. Mastery of these skills is essential for developing formulations that improve drug solubility and bioavailability.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Enhancing solubility and stability of poorly soluble drugs.’. Further sources in the context of Science might help you critically compare this page with similair documents:
First Pass Metabolism, Bioavailability of drug, Solid Dispersion, Aqueous solubility, Biopharmaceutics Classification System, PH adjustment, Complexation, Inclusion complex, Cyclodextrin, Poorly soluble drug, Solubility properties, Degradation process.