Optimizing inclusion complexes with an anti-diabetic drug

| Posted in: Science

Journal name: World Journal of Pharmaceutical Research
Original article title: Systematic optimization of formulation of inclusion complexes containing an anti-diabetic drug
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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Original source:

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Author:

Nirmala P., Marina Koland and Narendra C.


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Systematic optimization of formulation of inclusion complexes containing an anti-diabetic drug

Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research

Doi: 10.20959/wjpr20173-7929


Download the PDF file of the original publication


Summary of article contents:

Introduction

Glipizide (GZ) is a second-generation sulfonylurea used in the management of type II diabetes. As a BCS class II drug, it exhibits poor water solubility, which limits its bioavailability. To address this issue, the study explores the formulation of inclusion complexes using hydroxypropyl-β-cyclodextrin (HPβCD) through various methods, including physical mixture and solvent evaporation. The primary objective is to enhance the solubility and subsequent dissolution rate of Glipizide, thus improving its therapeutic effectiveness.

Impact of Excipients on Solubility Enhancement

The study assesses the impact of various excipients—PEG 10000, PVP K30, and PEG 6000—on the solubility of Glipizide. Phase solubility studies revealed that HPβCD significantly enhances the drug's solubility by 9.5-fold, while PVP K30 and PEG 6000 only offered a modest increase of fourfold and 3.8-fold respectively. The factorial design of experiments applied highlighted the interactive effects of the excipients, indicating that HPβCD alone provided the most substantial solubility enhancement. The intricate relationships between different excipients were clearly demonstrated, emphasizing the importance of selecting appropriate formulation components.

Techniques for Characterizing Inclusion Complexes

Various characterization techniques confirmed the formation of inclusion complexes. Fourier Transform Infrared Spectroscopy (FTIR) displayed significant changes in the spectral peaks of Glipizide when complexed with HPβCD, indicating altered molecular interactions. Differential Scanning Calorimetry (DSC) further supported this, showing the disappearance of the drug's melting point peak in the inclusion complex, which signified a reduction in crystallinity. Additionally, both 1H NMR and X-ray Diffraction (XRD) analyses corroborated the concept of complexation through the observation of reduced peak intensity and a shift in peak patterns, respectively.

Dissolution Studies and Their Implications

The dissolution studies highlighted the practical significance of the inclusion complexes. Compared to pure Glipizide and physical mixtures, the inclusion complex demonstrated a significant improvement in drug release rates. This finding underscores the efficacy of using HPβCD in drug delivery systems to facilitate enhanced solubility and that the method of delivery (e.g., encapsulation) can influence release kinetics. The release profiles indicated that the complexed form of GZ could provide a more immediate therapeutic effect, which is particularly beneficial in managing blood glucose levels in diabetic patients.

Conclusion

The study concludes that the inclusion of Glipizide with HPβCD through solvent evaporation is a promising strategy for improving its solubility and dissolution rate. The various characterization techniques confirmed the formation of inclusion complexes, while the dissolution studies illustrated their potential for enhanced therapeutic efficacy. This research highlights the necessity of utilizing suitable excipients and techniques in pharmaceutical formulations, particularly for poorly soluble drugs like Glipizide, to optimize their performance and therapeutic application.

FAQ section (important questions/answers):

What is the aim of the study involving Glipizide?

The study aims to formulate inclusion complexes of Glipizide with hydroxypropyl-β-cyclodextrin to improve its aqueous solubility and dissolution rate, thereby enhancing its bioavailability for diabetes treatment.

What methods were used to prepare the Glipizide inclusion complexes?

The Glipizide inclusion complexes were prepared using two methods: a physical mixture method and a solvent evaporation method. Both methods aimed to achieve optimal solubility enhancement of the drug.

How does HPβCD affect Glipizide’s solubility?

Hydroxypropyl-β-cyclodextrin (HPβCD) significantly enhances the solubility of Glipizide, achieving an approximate 9.5-fold increase, making it a highly effective excipient for this poorly water-soluble drug.

What characterization techniques were used in the study?

The study utilized various characterization techniques including FTIR, DSC, H NMR, and XRD to confirm the formation of inclusion complexes and to analyze their physical properties.

What were the dissolution study results of Glipizide’s complexes?

The dissolution studies revealed that the inclusion complex significantly improved drug release compared to both the physical mixture and pure Glipizide, indicating enhanced solubility and bioavailability.

What conclusion was drawn about HPβCD in the study?

The study concluded that HPβCD effectively enhances the solubility and drug release of Glipizide, establishing it as a crucial component for formulating this antidiabetic drug.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Optimizing inclusion complexes with an anti-diabetic drug”. 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 a substance used for medical treatment, particularly to relieve symptoms, cure diseases, or improve health. In this study, Glipizide is a significant drug being formulated to enhance its solubility and bioavailability for better treatment of type II diabetes, emphasizing the importance of drug formulation in pharmacotherapy.

2) Nirmala:
'Nirmala' is the name of the lead author of the research article, indicating her contribution to the field of pharmaceutical sciences. Recognized for her expertise, she spearheads studies focusing on enhancing drug formulations, particularly in the context of using cyclodextrins, paving the way for innovations in diabetes treatment.

3) Table:
In a scientific context, 'Table' refers to a method of organizing data in rows and columns for easier analysis and understanding. In this article, tables are used to present experimental results, calibration data, and findings from phase solubility studies, helping readers visualize essential information systematically.

4) Water:
'Water' is referred to as a solvent in pharmaceutical formulation, often used to dissolve drugs or as a medium in various experiments. It is crucial in the study of Glipizide's solubility, dissolution profile, and preparation of inclusion complexes with cyclodextrins, thus influencing drug delivery efficacy.

5) Study (Studying):
'Study' signifies the systematic investigation conducted to explore a particular topic—in this case, the optimization of Glipizide formulation. This research evaluates various methods like solvent evaporation and physical mixing for drug complexation to enhance solubility and therapeutic action, contributing to the field of pharmaceutical research.

6) India:
'India' denotes the geographic and cultural context in which the research was carried out. The study institutions and authors hail from India, specifically Karnataka, contributing to the global scientific community by addressing local and international health issues through pharmaceutical innovations, particularly in diabetes management.

7) Karnataka:
'Karnataka' is a state in India where the research and development activities for this study took place. The mention of Karnataka highlights the role of local pharmaceutical institutions in advancing drug formulation techniques, influencing the broader medical landscape in India and the global pharmaceutical industry.

8) Powder:
'Powder' refers to a finely ground material, often used in pharmaceutical formulations. This study involves the preparation of drug inclusion complexes where Glipizide and excipients are powdered and blended to promote further solubility enhancement, emphasizing the critical nature of powder characteristics in drug formulation.

9) Science (Scientific):
'Scientific' pertains to the rigorous, methodical approach that characterizes research in this field. The article embodies scientific principles by employing standardized methodologies and data analysis techniques in the study of Glipizide formulations, ensuring credibility and relevance in pharmaceutical sciences.

10) Medium:
'Medium' pertains to the environment in which a reaction or experiment occurs. In the context of this study, dissolution studies were conducted in water as the medium, influencing the solubility and release characteristics of Glipizide, making medium choice critical in pharmaceutical research.

11) Life:
'Life' refers to the biological processes of living organisms, where the significance of drug interventions becomes paramount. Glipizide's purpose as an antidiabetic agent illustrates the connection between medicinal chemistry and enhanced quality of life through effective disease management, underscoring relevance in healthcare.

12) Transformation (Transform, Transforming):
'Transform' refers to the process of changing the characteristics of a drug through formulation techniques. The study transforms Glipizide's solubility profile, showcasing innovative methods such as inclusion complex formation to enhance drug characteristics vital for therapeutic success.

13) Calculation:
'Calculation' pertains to the quantitative analysis performed during experiments. In the study, calculations involve determining the solubility of Glipizide using various factors and excipients, ensuring meticulous accuracy in assessing the effectiveness of formulated inclusion complexes to enhance therapeutic outcomes.

14) Performance:
'Performance' relates to how well a drug formulation achieves desired effects, such as enhanced solubility or faster dissolution. The study carefully evaluates the performance of Glipizide when combined with HPβCD to streamline its efficacy, a critical factor in optimal drug formulation.

15) Discussion:
'Discussion' refers to the section of the research where findings are interpreted and implications analyzed. In this article, the discussion contextualizes the results, addresses potential mechanisms of action for the observed solubility improvements, and suggests future research directions in drug formulation technology.

16) Narendra (Nara-indra):
'Narendra' is one of the co-authors of the study, contributing to the research team's collective efforts in investigating Glipizide formulations. His involvement represents the collaborative nature of scientific research, combining expertise to foster advancements in drug delivery systems.

17) Activity:
'Activity' typically refers to the biological effect a drug exerts within the body. Analysis of Glipizide’s activity upon formulation changes is crucial for recognizing how solubility improvements can enhance its ability to lower blood glucose levels effectively, resonating with therapeutic goals.

18) Channel:
'Channel' may refer to methods or pathways through which drugs are delivered or absorbed. In the context of this research, understanding the channeling of Glipizide's enhanced solubility through various formulations is imperative for optimizing its bioavailability and therapeutic effects.

19) Heating:
'Heating' indicates a method used during the solvent evaporation technique in drug formulation. In this study, controlled heating helps facilitate the dissolution of Glipizide and HPβCD, emphasizing thermal processes' significance in creating effective inclusion complexes and their relevance in pharmaceutical development.

20) Nature:
'Nature' signifies the intrinsic characteristics of substances, including drugs. The study focuses on the nature of Glipizide, particularly its hydrophobic properties and their impact on solubility, underscoring how understanding a drug's nature is fundamental in developing effective formulations.

21) Reason:
'Reason' pertains to the rationale behind conducting this study. The research aims to address the critical issue of Glipizide's poor solubility and bioavailability to improve its clinical utility, showcasing the need for optimized formulations to enhance treatment for type II diabetes.

22) Pitha:
'Pitha' refers to a significant researcher noted for contributions in the domain of cyclodextrins and drug formulations. Cited in the study, his work aids in contextualizing the methodology for utilizing HPβCD in improving the solubility of Glipizide in pharmaceutical applications.

23) Pulse:
'Pulse' in this context typically indicates a physical parameter, such as blood pulse, which is relevant in understanding drug effects like Glipizide’s. The drug's efficacy in regulating blood glucose levels can relate to various physiological functions, including circulation and metabolic responses.

24) Blood:
'Blood' signifies an essential bodily fluid that plays a crucial role in the administration and effects of drugs like Glipizide. The focus on Glipizide's ability to lower blood sugar levels illustrates the critical relationship between medication efficacy and patient health outcomes.

25) Beta:
'Beta' may refer to the beta cells in the pancreas, responsible for insulin production. Glipizide stimulates these cells, emphasizing the drug's therapeutic mechanism in lowering blood sugar levels for type II diabetes, making this concept pivotal in the study.

26) Pari:
'Pari' likely refers to a name or a specific reference within the study or contributing author. The relevance stems from collaborative efforts in research that illustrate the interconnected nature of scientific inquiry, contributing to evolving pharmaceutical knowledge and advancements.

27) Rich (Rch):
'Rich' in this context might describe the quality of composition or properties of a drug formulation, such as its content or solubility enhancements. Emphasizing rich formulations could convey the importance of complexing agents like HPβCD for improved therapeutic efficacy.

28) Line:
'Line' refers to a graphical representation typically used in data visualization, such as phase solubility or performance graphs to illustrate trends. Data lines provide insights into solubility changes with varying excipient concentrations, facilitating understanding of complex interactions in drug formulation.

Other Science Concepts:

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Discover the significance of concepts within the article: ‘Optimizing inclusion complexes with an anti-diabetic drug’. Further sources in the context of Science might help you critically compare this page with similair documents:

High performance liquid chromatography, Bioavailability, Fourier transform infrared spectroscopy, Differential scanning calorimetry, X-ray diffraction studies, UV-Spectroscopy, Dissolution studies, Excipient, Anti-diabetic drug.

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