Colon-targeted drug delivery design for lornoxicam evaluation.

| Posted in: Science

Journal name: World Journal of Pharmaceutical Research
Original article title: Design, formulation and evaluation of colon targeted drug deluivery of lornoxicam
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:

R. B. Desireddy, Ch. Sunil Kumar, S. K. Salman, T. Vinod Kumar, T. Eswar Sai and Badri Kumar


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Design, formulation and evaluation of colon targeted drug deluivery of lornoxicam

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

Doi: 10.20959/wjpr20185-11391


Download the PDF file of the original publication


Summary of article contents:

Introduction

The research study conducted by R. B. Desireddy and his colleagues aimed to develop colon-targeted tablets of the non-steroidal anti-inflammatory drug, lornoxicam. The formulation utilized various polymers, specifically Hydroxypropyl Methylcellulose (HPMC) and Ethyl Cellulose, to enhance targeted drug delivery to the colon. This approach is particularly relevant due to the limitations associated with conventional oral drug formulations, which often require multiple dosing and suffer from low bioavailability due to gastrointestinal degradation and first-pass metabolism.

Development of Colon Targeted Formulations

The formulation process involved creating enteric press-coated lornoxicam tablets, beginning with a rapid release core tablet infused with different superdisintegrants. The study explored the formulation of these core tablets through direct compression, ensuring optimal physical parameters such as hardness and friability. The use of superdisintegrants like Crospovidone and Sodium Starch Glycolate aimed to facilitate swelling upon reaching the colon, thereby ensuring a controlled and effective release of lornoxicam. Over nine unique formulations were tested, ultimately identifying one formulation, F6, as the most promising based on in-vitro dissolution results.

Importance of Polymer Composition

A crucial aspect of the study was the interaction between the drug and the selected polymers. The researchers discovered that higher concentrations of HPMC led to a retarded release rate of lornoxicam, as the drug could become entrapped within the polymer matrix. Consequently, the right balance of HPMC and Ethyl Cellulose was essential to achieve the desired colon-targeted drug release. The combination of these polymers allowed for greater flexibility in modifying the drug release profile, thereby improving the therapeutic efficacy and reducing gastrointestinal side effects often associated with frequent dosing.

Evaluation of Drug Release Profiles

In-vitro dissolution studies were central to evaluating the performance of the drug formulations. The results indicated that the cumulative drug release for the rapid release core tablets over 12 hours ranged from 75% to 98.4%. The polymer composition significantly influenced the release rates, where lower levels of HPMC enhanced drug release compared to higher concentrations that impeded it. The study also confirmed that the enteric press-coated tablets could sustain drug release even in acidic environments, promoting localized delivery to the colon.

Conclusion

The research concluded that the formulated colon-targeted tablets of lornoxicam, utilizing HPMC and Ethyl Cellulose, demonstrated potential for enhanced drug delivery to the colonic region. By carefully manipulating the polymer combinations and their concentrations within the formulation, the study offered a viable approach to overcome challenges associated with conventional drug delivery methods. This development could improve patient compliance by reducing the frequency of dosing while maintaining therapeutic effectiveness, thereby presenting a significant advancement in gastroenterology.

FAQ section (important questions/answers):

What was the aim of the research on Lornoxicam?

The research aimed to develop colon-targeted tablets of Lornoxicam using HPMC and Ethyl cellulose as polymer carriers to improve drug delivery, enhance therapeutic efficacy, and minimize gastrointestinal disturbances.

What polymers were used in the Lornoxicam tablets?

The study used Hydroxypropyl Methylcellulose (HPMC) and Ethyl cellulose in various concentrations to create matrix tablets for colon-targeted drug delivery.

How were the formulations evaluated?

Formulations underwent several pharmacopoeial tests, including hardness, friability, thickness, drug content, weight variation, and in-vitro drug release studies to ensure quality and performance.

What method was used to prepare the tablets?

The tablets were prepared using the direct compression method, which is a widely used technique in pharmaceutical manufacturing for solid dosage forms.

Why is colon-targeted delivery important for Lornoxicam?

Colon-targeted delivery is essential to ensure that Lornoxicam reaches the site of action effectively, enhancing its therapeutic effect while reducing side effects associated with gastrointestinal tract exposure.

What were the main findings of the dissolution studies?

The dissolution studies indicated that Lornoxicam release rates were influenced by polymer concentrations; formulations with lower HPMC concentrations showed higher drug release compared to those with higher concentrations.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Colon-targeted drug delivery design for lornoxicam evaluation.”. 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 'drugs' refers generically to substances used for medical treatment. This study specifically looks at drugs such as lornoxicam to address conditions that may warrant advanced drug delivery systems. The discussion around different types of drugs underlines the importance of tailoring pharmacological approaches to meet specific therapeutic needs.

2) Table:
In the context of pharmaceutical research, a 'table' often implies a structured presentation of data, including formulations, experimental results, or evaluations. Tables provide clear comparative insights regarding the compositions and properties of drug formulations, such as those developed for colon-targeted delivery of lornoxicam, facilitating easier understanding and analysis of results.

3) Disease:
The term 'diseases' represents various health conditions that affect individuals, particularly chronic illnesses. This study addresses specific diseases affecting the colon, underscoring the need for innovative drug delivery techniques that ensure better treatment efficacy and reduce the frequency of administration, ultimately enhancing patient quality of life.

4) India:
India is the country where the research was conducted, indicating the geographic context of the study. Its rich pharmaceutical landscape contributes to the drug development process, fostering innovations like colon-targeted formulations. The study's setting within India highlights regional health issues and the quest for effective treatments in local populations.

5) Kumar:
This name likely refers to Ch. Sunil Kumar, the corresponding author of the study. The inclusion of authors' names is critical for academic accountability, allowing for credit attribution in research studies. Kumar's work contributes to the ongoing exploration of targeted drug delivery systems, specifically regarding lornoxicam, in pharmacological research.

6) Study (Studying):
The term 'study' refers to a systematic investigation aimed at contributing new knowledge or validating existing knowledge within a specific scientific field. In this piece, it denotes the research work focused on developing and evaluating colon-targeted formulations of lornoxicam, indicating the goal of enhancing drug delivery and therapeutic effectiveness.

7) Post:
In a research context, 'post' can indicate stages following a specific event or phase of study. In this document, it likely refers to 'post-compression' parameters, essential in evaluating the physical characteristics of tablets after they have been formed, impacting the overall quality and efficacy of drug delivery systems.

8) Science (Scientific):
Science signifies the systematic pursuit of knowledge through observation and experimentation. In this research, the application of scientific principles is evident in the design, formulation, and evaluation of colon-targeted drug delivery systems. It showcases the intersection of pharmacology and pharmaceutical sciences to improve therapeutic outcomes.

9) Nalanda (Nalamda):
Nalanda refers to the Nalanda Institute of Pharmaceutical Sciences, the institution where the research was conducted. The name is relevant as it indicates the credibility of the research work, suggesting that it is rooted in an educational environment focused on pharmaceutical advancements and contributing to broader medical sciences.

10) Andhra (Amdhra):
'Andhra' pertains to Andhra Pradesh, the Indian state where the research was conducted. Including this geographic detail emphasizes local health challenges and the context of drug formulation development. It positions the study within regional healthcare frameworks, potentially benefiting local populations facing specific health issues related to the colon.

11) Reason:
In the context of scientific research, 'reason' signifies the rationale or justification behind conducting a study. This research is driven by the need to improve drug availability and targeting, particularly for conditions involving the colon. Understanding patient compliance issues also drives the motivation for innovative therapeutic strategies.

12) Medium:
In pharmaceutical studies, 'medium' often refers to the solution or environment in which drug release and dissolution studies are carried out. In this research, various pH mediums are used to mimic physiological conditions, crucial for assessing the performance of lornoxicam formulations and their behavior in targeted delivery.

13) Powder:
'Powder' indicates a form of pharmaceutical ingredient utilized in tablet formulation. The study includes various powders like microcrystalline cellulose and excipients, which are essential for the mechanics of tablet formation, ensuring the final product's stability, drug release characteristics, and overall performance in therapeutic applications.

14) Discussion:
In research, the 'discussion' section typically interprets the study's findings, highlighting their significance and implications. This document's discussion likely addresses the effectiveness of the colon-targeted formulations, comparing results with existing literature, which helps contextualize the contribution of the study to current scientific understanding.

15) Developing:
The term 'developing' encapsulates the continuous process of creating and improving formulations, drugs, or technologies. In this context, it refers to the design and optimization of colon-targeted delivery systems for lornoxicam, emphasizing innovation in addressing therapeutic challenges associated with conventional drug administration methods.

16) Activity:
The term 'activity' often relates to the pharmacological effects a drug has within the body. This study seeks to enhance the activity of lornoxicam by employing targeted delivery methods, aiming to adjust its release profile, maximize bioavailability, and optimize its therapeutic impact, particularly in treating colonic diseases.

17) Bleeding:
'Bleeding' can refer to a serious medical condition that may arise from underlying diseases affecting the gastrointestinal tract. Researching drug formulations like lornoxicam includes considerations to minimize side effects like gastrointestinal bleeding, enhancing patient safety and efficacy by avoiding excessive drug accumulation in sensitive areas.

18) Chandra:
'Chandra' likely refers to Chandra Labs, a source of materials for this research. This term signifies collaboration and support from external entities in the pharmaceutical development process, reflecting the importance of partnerships in advancing research work and methodologies in the field of drug delivery systems.

19) Ulcer:
'Ulcer' denotes a specific medical condition that involves the erosion of the skin or mucous membrane. The relevance in this study highlights the need for drug delivery systems that address conditions like peptic ulcers, particularly concerning anti-inflammatory medications such as lornoxicam that target gastrointestinal disorders.

20) Bell:
'Bell' is not explicitly referenced in the provided context, but generally, it could signify recognition of significant aspects related to research or discoveries. It could also symbolize alertness within the pharmaceutical field, emphasizing the importance of remaining aware of advancements and challenges in drug development.

21) Life:
'Life' pertains to the holistic aspect of health and well-being. In this research context, improved drug delivery methods aim to enhance the quality of life for patients by ensuring effective treatment of chronic conditions while providing significant therapeutic benefits and reducing the burden of medication adherence.

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