Formulation and evaluation of gatifloxacin topical semisolid dosage forms

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Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and evaluation of gatifloxacin topical semisolid dosage forms
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:

Mohamed A. El-Nabarawi, Ahmed H. El-Shafai and Dina M. Mahmoud Abdelfattah


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Formulation and evaluation of gatifloxacin topical semisolid dosage forms

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

Copyright (license): WJPR: All rights reserved


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Summary of article contents:

Introduction

This study aimed to develop and evaluate semisolid formulations of Gatifloxacin, a fluoroquinolone antibiotic, in the form of gels and emulgels with optimal rheological and release characteristics. Gatifloxacin is used topically for treating bacterial conjunctivitis, and its delivery system was designed to enhance localized therapeutic effects while bypassing systemic absorption. The formulations were tested for various physical and chemical properties, including viscosity, drug release rates, and bioadhesion, using different concentrations and types of gelling and emulsifying agents.

The Importance of Scalable Drug Release

One critical finding of the study was the relationship between polymer concentration and drug release kinetics. As the concentration of polymers in the formulations increased, the release rates of Gatifloxacin tended to decrease. This is attributed to the increased viscosity and density of the polymer network, which restricts the movement of the drug, thereby creating a diffusion barrier. Notably, formulations containing 2% sodium carboxymethylcellulose (SCMC) exhibited the highest drug release rates, while those with higher concentrations of polymers resulted in lower release percentages. This relationship underscores the need for careful selection of polymer concentrations in designing topical formulations to achieve the desired therapeutic effect.

Rheological Properties and Their Significance

The study also highlighted that the rheological properties of the formulations correlated with their performance in drug delivery. All semisolid formulations were characterized by non-Newtonian, pseudoplastic flow behavior and exhibited thixotropic properties. Such behavior is essential because it allows the formulation to be easily spreadable upon application, while regaining its viscosity afterward, maintaining stability. Carbopol 934-based formulations were noted for their higher viscosities compared to those made with cellulose derivatives, emphasizing the significance of gelling agents in achieving desirable texture and performance in topical applications.

Evaluation of Bioadhesive Strength

Another significant aspect of the study was the evaluation of bioadhesive strength of the formulations, which reflects their ability to adhere to the skin and prolong drug retention at the application site. The results indicated that most formulations demonstrated satisfactory bioadhesive strengths. Formulation FEg7, in particular, had the lowest bioadhesive strength while maintaining acceptable spreadability and extrudability. This balance suggests that optimal bioadhesion is crucial in enhancing the duration of drug action, essential for effective treatment in topical applications.

Conclusion

In conclusion, the research successfully formulated different semisolid dosage forms of Gatifloxacin, with FEg7 identified as the most suitable for topical applications due to its favorable drug release profile and physical characteristics. The study emphasizes the critical roles of polymer selection, rheological properties, and bioadhesion in developing effective topical drug delivery systems. Future formulations can leverage these findings to enhance therapeutic efficacy and patient compliance in topical drug administration.

FAQ section (important questions/answers):

What is the main purpose of formulating Gatifloxacin in this study?

The study aims to formulate Gatifloxacin in different semisolid preparations such as gels and emulgels with optimal rheological and release properties for effective topical delivery.

How does Gatifloxacin function as an antibiotic?

Gatifloxacin inhibits bacterial enzymes DNA gyrase and topoisomerase IV, effectively treating bacterial conjunctivitis. Its design aims to minimize microbial resistance.

What are the physical properties evaluated for the formulations?

Physical properties like appearance, color, homogeneity, odor, gelling capacity, and viscosity are assessed to ensure the formulations are suitable for topical applications.

How were the emulgel formulations prepared in this study?

Emulgel formulations were prepared by mixing gelling agents, liquid paraffin, and emulsifiers, adjusting pH, heating phases, and then creating a gel-emulsion blend.

What method was used for evaluating drug release from the formulations?

In vitro drug release was assessed using the modified USP dissolution apparatus, measuring the cumulative amount of Gatifloxacin released over time.

Which emulgel formulation was found most effective for topical application?

Formulation F_Eg7 demonstrated the highest drug release and optimal physical properties, making it the most suitable option for topical applications.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Formulation and evaluation of gatifloxacin topical semisolid dosage forms”. 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:
A drug is a chemical substance that interacts with the body to produce a physiological effect. In the context of this study, Gatifloxacin is the drug being formulated into topical forms. Understanding the properties and release of drugs is crucial for effective treatment of various diseases and conditions.

2) Table:
A table is a structured arrangement of data organized into rows and columns, often used in scientific articles to present experimental results, formulations, or comparisons. In this study, tables display formulations, physical properties, and evaluation results, facilitating easy comparison and understanding of experimental findings.

3) Water:
Water is a universal solvent and a crucial medium for many chemical processes, including drug formulation. In this study, water is used to wet gel bases and dissolve the drug Gatifloxacin, demonstrating its importance in creating effective topical formulations that enhance drug delivery and bioavailability.

4) Fainting (Fainted):
The term faint refers to a color that is light or pale. In this study, formulations exhibited faint yellow or faint yellowish-green colors, which indicate their composition and appearance. Color characteristics can influence the aesthetic appeal of a topical product, impacting user perception and acceptance.

5) Study (Studying):
A study refers to a systematic investigation aimed at discovering or interpreting facts, theories, or general principles. The research presented in this document investigates the formulation and evaluation of Gatifloxacin topical preparations, contributing to the field of pharmaceutical sciences by exploring drug delivery systems.

6) Swelling:
Swelling pertains to the increase in size or volume of a substance when it absorbs water or another solvent. In the context of topical gels and emulgels, swelling affects drug release and bioadhesion properties, which are essential for effective penetration and therapeutic action on the skin.

7) Measurement:
Measurement is the determination of the size, quantity, or degree of something. In this study, various parameters such as pH, viscosity, drug content, and bioadhesive strength are measured to evaluate the quality and performance of Gatifloxacin formulations, ensuring they meet required standards for topical application.

8) Medium:
In this context, medium refers to the substance in which drug release and permeation take place. The phosphate buffer used in the experiments acts as a medium for drug diffusion studies, simulating physiological conditions to better understand how the drug interacts with biological barriers.

9) Glass:
Glass is a common material utilized in scientific settings for laboratory equipment such as beakers, test tubes, and watch glasses. In this study, glass containers are used to hold and measure different formulations, facilitating observations during in vitro release and permeation tests.

10) Relative:
Relative refers to something considered in relation to something else. In this study, the relative permeation rate assesses how the Gatifloxacin formulation compares to control formulations. Understanding relative values allows researchers to identify superior formulations based on their efficacy in drug delivery.

11) Surface:
Surface denotes the outermost layer of a material. In this research, the surface of skin or membranes is critical in topical applications as it relates to how well drugs can permeate into deeper layers. Surface interactions significantly influence the effectiveness of topical therapies.

12) Egypt:
Egypt, where the research was conducted, is significant in this context as it establishes the geographical and cultural context of pharmaceutical studies. The country's educational institutions, like Cairo University, contribute to the global landscape of pharmaceutical research through innovative works such as this formulation study.

13) Antibiotic (Antibacterial):
An antibiotic is a type of medication used to treat bacterial infections by inhibiting the growth or killing bacteria. Gatifloxacin, the antibiotic studied here, belongs to the fluoroquinolone family, and its formulation into topical preparations addresses the localized treatment of various bacterial skin infections.

14) Substance:
A substance is a form of matter with a specific composition and properties. In pharmaceuticals, the term refers to the active ingredients and excipients in formulations. The study focuses on substances like Gatifloxacin and various polymers used to ensure effective drug delivery in topical applications.

15) Company:
A company is a legal entity that engages in commercial, industrial, or professional activities. The study references specific companies such as Sigma Chemical Company, highlighting the sources of raw materials used in formulations. This underscores the relevance of industry collaborations in pharmaceutical research.

16) Pharmacological:
Pharmacological relates to the branch of medicine concerned with the uses, effects, and mechanisms of action of drugs. Understanding pharmacological properties is essential for evaluating drug formulations like Gatifloxacin, ensuring their effectiveness and safety in treating specific conditions and diseases.

17) Discussion:
Discussion refers to the section of a research paper where results are interpreted and implications are analyzed. This part of the study evaluates findings, compares them to existing literature, and draws conclusions regarding the effectiveness of Gatifloxacin formulations for topical applications.

18) Activity:
Activity in pharmacology refers to the effect a drug has on biological systems. In this study, the activity of Gatifloxacin against bacteria is of primary concern. Understanding the activity helps determine the optimal formulation that maximizes therapeutic effects while minimizing side effects.

19) Disease:
Disease signifies a pathological condition of a bodily part resulting from various causes. The study focuses on conditions that antibiotics like Gatifloxacin can treat, enhancing our understanding of how specific topical formulations can effectively manage bacterial infections and associated skin ailments.

20) Thomas:
Thomas likely refers to a company or entity involved in providing materials, such as membranes used in experiments. Identifying sources like Thomas Company emphasizes the importance of validated materials in ensuring the reliability and reproducibility of pharmaceutical research.

21) Family:
Family refers to a group of related organisms or chemical entities. In pharmacology, understanding the family of a drug, such as fluoroquinolones in the case of Gatifloxacin, helps researchers establish pharmacological relationships and predict the behavior of drugs based on their similar chemical structure.

22) Powder:
Powder denotes a form of substance consisting of fine, dry particles. In pharmaceuticals, formulations may include powdered excipients that assist in creating hydrogels or emulsifying agents essential for designing effective topical drug delivery systems, enhancing stability and drug release.

23) Filling (Filled):
Filled refers to the process of adding one substance into another. In the context of this research, the term may describe the preparation of formulations where the drug is incorporated into a gel or emulgel, ensuring even distribution and optimal therapeutic efficacy.

24) Dina:
Dina is likely one of the authors involved in the research study. By highlighting contributors, the text recognizes individual efforts in the study, emphasizing teamwork and collaboration in the field of pharmaceutical sciences toward achieving a common goal of effective drug formulation.

25) Tear:
Tear refers to the fluid produced by the lacrimal glands, crucial for eye health. In the study, simulated tear fluid is used to test gelling capacities of formulations that may be applied to treat conditions like bacterial conjunctivitis, emphasizing the importance of mimicking physiological conditions.

26) Pain:
Pain signifies an uncomfortable sensation signaling injury or illness. In the context of topical drug formulations, effective management of pain (for instance, in conditions like psoriasis) is essential. Understanding how formulations alleviate pain is vital for designing user-friendly and effective therapeutic products.

27) Hand:
Hand refers to the part of the body reaching into many manual activities, implicitly signifying the importance of ease of application for topical formulations. Considering the user's hand in product design ensures that medications can be readily applied to areas requiring treatment, enhancing user compliance.

Other Science Concepts:

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Discover the significance of concepts within the article: ‘Formulation and evaluation of gatifloxacin topical semisolid dosage forms’. Further sources in the context of Science might help you critically compare this page with similair documents:

Topical application, Semisolid preparations, Analytical grade, PH measurement, Organoleptic properties, First Pass Metabolism, Statistical study, Emulsifying agent, Swelling Index, Gel formulation, Spectrophotometric estimation, Gelling agent, Cutaneous disorders.

Concepts being referred in other categories, contexts and sources.

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