Aceclofenac transdermal gel: herbal extract for enhanced penetration.
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation, optimization and evaluation of aceclofenac transdermal gel- a novel approach for penetration enhancement by herbal extract
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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Singh Rampal, Juyal Divya, Singh Vikram and Rawat Geeta
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation, optimization and evaluation of aceclofenac transdermal gel- a novel approach for penetration enhancement by herbal extract
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
The research detailed in this article focuses on the formulation, optimization, and evaluation of a transdermal gel containing aceclofenac, a non-steroidal anti-inflammatory drug (NSAID) known for its analgesic and anti-inflammatory properties. The study incorporates the use of herbal extracts, specifically oil derived from Acorus calamus, to enhance the permeability of the drug across the skin barrier. Various excipients, such as carbopol 941 P, HPMC K15 M, propylene glycol, triethanolamine, and methyl paraben, are utilized in the formulation process, with evaluations conducted to assess the gel's pH, spreadability, extrudability, viscosity, drug content, and in vitro permeability.
Penetration Enhancement through Herbal Extracts
A key finding of the study is the significant role of Acorus calamus oil as a penetration enhancer in the transdermal gel formulation. The oil was incorporated into different gel formulations at varying concentrations. The results demonstrated that as the concentration of Acorus calamus oil increased, the drug release rate of aceclofenac also increased. Specifically, the highest concentration of 5 ml of the herb-derived oil yielded optimal results with a cumulative drug release of 66.78% over six hours, which was substantially higher than the 21.00% drug release observed in the plain gel formulation. This highlights the effectiveness of herbal oils in enhancing drug penetration through the skin, potentially leading to improved therapeutic outcomes.
Formulation and Evaluation Parameters
The evaluation of the prepared gel formulations highlighted several critical parameters. The pH values of the various gel formulations ranged from 6.80 to 7.23, indicating skin compatibility. Spreadability, which measures the ease of application, varied between 11.66 and 14.66 g.cm/sec, suggesting that the gels were easy to spread on the skin. Moreover, extrudability, quantifying the force required to dispense the product, ranged from 250.00 to 444.44 g.cm². The viscosity of the gels, indicating the thickness and flow properties, was also significant, with values between 21,023 cps to 22,101 cps. These evaluations demonstrated that the formulations were suitable for topical application, meeting the desirable characteristics of a transdermal delivery system.
Drug Release Kinetics and Stability Studies
The kinetic analysis of the drug release from the gels suggested that the formulations containing Acorus calamus oil followed a diffusion-controlled release pattern, fitting best with the Higuchi diffusion model and displaying a correlation coefficient (R²) of 0.948. This insight into the drug release mechanism is crucial as it informs the potential efficacy and bioavailability of aceclofenac when delivered transdermally. Furthermore, stability studies performed under varying temperature conditions (4°C, 25°C, and 40°C) over a 15-day period indicated no significant changes in the physical appearance, pH, or drug content of the gel formulations. This suggests that the gels maintained their integrity and efficacy over time, critical for commercial viability.
Conclusion
The study successfully developed a transdermal gel formulation of aceclofenac enhanced with Acorus calamus oil, demonstrating improved drug release profiles and stability. The incorporation of herbal extracts not only facilitates better drug permeability but also reflects a growing trend towards utilizing natural ingredients in pharmaceutical formulations. The promising results encourage further research into herbal-based drug delivery systems, potentially leading to more effective pain management therapies with fewer side effects compared to conventional oral medications. Overall, this research contributes to the emerging field of herbal pharmacotherapy and its applications in modern medicine.
FAQ section (important questions/answers):
What is the purpose of the research on aceclofenac gel?
The research aims to formulate, optimize, and evaluate a transdermal gel containing aceclofenac, enhanced with acorus calamus oil, focusing on improving the drug's penetration and release properties.
How does aceclofenac function as a medication?
Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) that alleviates pain and inflammation by inhibiting prostaglandin synthesis. It is effective for conditions like headaches, arthritis, and joint pain.
What are the evaluated properties of the aceclofenac gel?
The gel was evaluated for pH, spreadability, extrudability, viscosity, drug content, in vitro permeability, and drug-polymer compatibility using FTIR studies to ensure effective formulation.
What is the composition of the aceclofenac transdermal gel?
The gel consists of aceclofenac, carbopol 941, HPMC K15, propylene glycol, triethanolamine, methyl paraben, and acorus calamus oil, which enhances drug penetration.
What were the results of the drug release study?
The cumulative drug release from the gel formulations ranged from 48.50% to 66.78% over six hours, showing that gels with higher acorus calamus concentration released more drug.
What methods were used for oil extraction from acorus calamus?
The essential oil was extracted using the Clevenger apparatus, utilizing distilled water at a temperature of 70-80°C for 6-8 hours, resulting in a light yellow oil.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Aceclofenac transdermal gel: herbal extract for enhanced penetration.”. 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 that is used for therapeutic purposes, specifically in this research involving aceclofenac, a non-steroidal anti-inflammatory drug (NSAID). The study aims to optimize transdermal delivery systems for drugs, enhancing their efficacy and minimizing adverse effects.
2) Acorus calamus:
Acorus calamus, or sweet flag, is a medicinal plant used in this research as a penetration enhancer in formulating aceclofenac transdermal gel. Its essential oils, especially β-asarone, are believed to improve drug absorption through the skin, demonstrating its relevance in herbal medicine and pharmaceutical formulations.
3) Rampal (Rāmpāl):
Rampal refers to one of the primary authors of the study who contributed to the formulation, optimization, and evaluation of the aceclofenac transdermal gel. His work reflects the importance of individual researchers in advancing pharmaceutical science and developing effective drug delivery systems.
4) Science (Scientific):
Science underlies the entire research publication, encompassing the systematic study of substances, their interactions, and the principles governing drug formulation and delivery. It highlights the application of scientific methods to evaluate drug efficacy, enhancing our understanding of pharmacology and medicinal chemistry within healthcare.
5) Water:
Water is used as a solvent in the extraction and preparation of the transdermal gel formulations. Its role is crucial as it enables the dissolution of various components, facilitating the uniform distribution of the active pharmaceutical ingredient (API) along with enhancing the gel's consistency and texture.
6) Table:
The 'Table' represents structured data within the publication, summarizing experimental results such as formulation compositions, evaluation parameters, and drug release profiles. Tables serve to present complex information concisely, aiding readers in comprehending and comparing different formulations and results.
7) Phytochemical:
Phytochemical refers to the chemical compounds produced by plants, particularly studied for their potential health benefits. In this research, phytochemical tests conducted on Acorus calamus help identify compounds that may contribute to its medicinal properties, such as saponins, tannins, and terpenoids.
8) Pain (Paiṇ):
Pain management is a significant focus of the research, given that aceclofenac is primarily used to alleviate various types of pain, including arthritis and inflammatory conditions. The study's goal is to enhance delivery methods to improve therapeutic outcomes and patient quality of life.
9) Glass:
Glass is mentioned in the context of laboratory equipment such as slides and beakers used during experiments. Its relevance lies in the material's inertness and clarity, which ensures accurate readings during measurements, such as during the viscosity tests and drug release evaluations.
10) Study (Studying):
The term 'Study' encompasses the research conducted to evaluate the effectiveness of a new formulation of aceclofenac in transdermal gel form. It reflects the scientific inquiry into drug development and formulation strategies, contributing valuable insights to pharmaceutical research.
11) New Delhi:
New Delhi is mentioned as the location of Central Drug House, a supplier of chemicals used in the formulations. Its inclusion highlights the geographical context of pharmaceutical supply chains and the importance of local resources in academic research and industrial applications.
12) Pharmacological:
Pharmacological refers to the study of how drugs interact within living organisms and their potential effects on health. This research emphasizes pharmacological principles in developing herbal formulations that can effectively target inflammation and pain through enhanced skin absorption.
13) Measurement:
Measurement is integral for obtaining quantitative data, such as viscosity, drug content, and pH levels in the gel formulations. Precise measurements ensure the reliability and reproducibility of results, which are crucial for assessing the quality and performance of pharmaceutical products.
14) Sweet flag:
Sweet flag is the common name for Acorus calamus, the plant studied for its medicinal properties. Its essential oils enhance drug absorption, making it key to the development of new transdermal delivery systems, reaffirming traditional knowledge in herbal medicine.
15) Sharman (Śarma, Sarmā, Sarma, Sharma, Śarman):
Sharma is referenced as a co-author related to the study, reflecting the collaborative nature of research. The involvement of multiple researchers highlights diverse expertise contributing to the successful formulation and optimization of the aceclofenac gel.
16) Indian:
Indian relates to the geographical and cultural context of the study, as Acorus calamus is native to India. This reflects the rich biodiversity and traditional medicinal practices present in the country, which are valuable in modern pharmacology and drug formulation.
17) Delhi:
Delhi, as a prominent city in India, serves as a hub for pharmaceutical research and academia. Its mention underlines the location's significance in scientific discourse and the development of healthcare solutions, particularly in the context of this study.
18) India:
India refers to the country from which the raw materials for the research were sourced. It represents a vast resource of medicinal plants and traditional knowledge, providing a rich background for exploring natural compounds in modern drug formulations.
19) Flag:
Flag refers to the common name 'sweet flag' for Acorus calamus, emphasizing the plant's cultural and historical significance. It underscores the integration of traditional herbal remedies into contemporary pharmaceutical research, embodying a fusion of ancient wisdom and modern science.
20) Rheumatoid arthritis:
Rheumatoid arthritis is a chronic inflammatory disorder for which aceclofenac is commonly prescribed. The study's focus on transdermal drug delivery systems aims to improve treatment efficacy for this condition, reflecting its clinical relevance in managing chronic pain and inflammation.
21) Curcuma longa:
Curcuma longa, known for its anti-inflammatory properties, is referenced as another herbal candidate utilized in medicinal formulations. Its relevance highlights the ongoing exploration of natural substances in pharmacotherapy, emphasizing the synergy between various plant extracts and their therapeutic potential.
22) Pharmacotherapy:
Pharmacotherapy encompasses the use of drugs to treat diseases and conditions. This research aims to enhance the pharmacotherapy of pain through improved drug delivery methods, illustrating the significance of effective medication management strategies in clinical practice.
23) Inflammation:
Inflammation is a biological response that aceclofenac aims to alleviate, and has relevance to the study's objective of optimizing formulations for faster drug delivery. Understanding inflammatory processes informs the development of effective pharmaceutical interventions to manage related conditions.
24) Discussion:
Discussion is the section of scientific papers where results are interpreted and contextualized. It is crucial for understanding the implications of findings, comparing with existing literature, and proposing future research directions in the field of drug formulation and delivery.
25) Composite:
Composite reflects the methodology used in formulating the gel, where various components are combined to achieve desired properties. This term emphasizes the integral nature of formulation science in creating effective delivery systems for pharmaceutical applications.
26) Tirupati (Thirupati, Tiruppaṭi):
Tirupati is referenced as the location of Tirupati Medicare Ltd, which supplied aceclofenac for the research. Its mention highlights the role of regional pharmaceutical companies in supplying active ingredients for academic investigations and product development.
27) Srinagar:
Srinagar, the location of H.N.B.G.U., is important as it represents the educational institutions contributing to pharmaceutical research in India. Its involvement underscores the academic collaboration and importance of research facilities in advancing drug development.
28) Vomiting:
Vomiting is one of the side effects associated with aceclofenac and other NSAIDs. The study's focus on transdermal delivery systems is to reduce gastrointestinal side effects, enhancing patient compliance and overall therapeutic experience.
29) Chandra:
Chandra refers to Dr. Anup Chandra, a taxonomist involved in identifying and authenticating the plant material. His role underscores the importance of proper identification of herbal sources in ensuring the efficacy and safety of the herbal formulations used in research.
30) Chennai:
Chennai, being a major city in India, is noted for sources of pharmaceutical products like Hifenac gel. Its mention highlights the geographical context of market availability and establishes a framework for comparing research formulations with commercially available options.
31) Surface:
Surface refers to the skin where the transdermal gel is applied. The study's emphasis on enhancing drug permeability through the skin surface illustrates the importance of formulation strategies for improving therapeutic outcomes.
32) Filling (Filled):
Filled denotes the final step in the formulation process, where the gel is placed into containers. Proper filling ensures that the gels are intended for medical use maintain their efficacy and safety until application.
33) Santha (Śaṇṭha, Saṃtha, Ṣaṇṭha, Sanṭha, Shantha, Santh):
Shantha is mentioned as a contributing author, signifying the collaborative efforts in research. The authors’ diverse expertise aids in the comprehensive development and validation of the transdermal gel formulation.
34) Camara (Cāmara, Camará):
Camara refers to Lantana camara, another plant that may have been considered for its medicinal properties. Its inclusion demonstrates the broad exploration of botanical sources for developing effective therapeutic formulations.
35) Rajput:
Rajput is another author involved in this research, reflecting the importance of a multidisciplinary approach in developing pharmaceutical formulations. Collaboration enriches the study with a variety of perspectives and expertise.
36) Forest:
Forest is referenced in the context of the collection and authentication of the plant samples. It highlights the importance of biodiversity and natural ecosystems in sourcing medicinal plants for pharmaceutical use.
37) Family:
Family refers to the taxonomical classification of plants. Understanding the family of Acorus calamus is essential for identifying its related species and potential medicinal properties, emphasizing the botanical framework of the study.
38) Nausea:
Nausea is another common side effect linked to aceclofenac. The research aims to develop transdermal formulations that minimize systemic exposure, thereby reducing the risk of gastrointestinal side effects like nausea.
39) Powder:
Powder refers to the form of plant materials used in phytochemical testing, emphasizing the importance of sample preparation in scientific evaluations. Properly prepared powders are crucial for accurate phytochemical analyses and subsequent formulation processes.
40) Saxena (Sakshena, Saksena):
Saxena, a contributor to the research, signifies teamwork in pharmaceutical development. His collaborative efforts contribute greatly to the collective knowledge essential for formulating effective therapeutic products.
41) Divya (Divyā):
Divya is a co-author involved in the research, reflecting the collaborative aspect of scientific inquiry. The inclusion of her expertise highlights the importance of teamwork in achieving comprehensive research outcomes.
42) Madra (Madrā):
Madra may refer to a source or context related to the research. Its association can signify the relevance of local resources and contributions to the pharmaceutical landscape in developing effective formulations.
43) Nanda (Nandā, Namda):
Nanda is mentioned as part of the research team, emphasizing the collaboration necessary for successful pharmaceutical investigations. Each team member contributes a unique skill set that enhances the overall research process.
44) Kumar (Kumār):
Kumar, as a contributor, reflects the collaborative effort in the research study. The team's collective expertise demonstrates the importance of diverse knowledge in effectively addressing complex pharmaceutical challenges.
45) Patel (Paṭel, Pāṭel):
Patel is referenced as an author involved in the study, underscoring the team dynamic and collaborative approach in pharmaceutical research. Each author's contributions reflect a synergy that enhances the study's depth and quality.
46) House:
House refers to Central Drug House, which supplied materials for the formulation. Highlighting suppliers showcases the interconnectedness of academia and industry in the pharmaceutical field, facilitating research and development.
47) Ras (Rās, Rash):
Rash is a potential skin reaction that may occur with topical medications, highlighting the importance of safety in drug formulations. The study's focus on biocompatibility and effectiveness aims to minimize adverse reactions in patients.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Aceclofenac transdermal gel: herbal extract for enhanced penetration.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Non steroidal anti inflammatory drug, Saponins Test, Stability Studies, Viscosity measurement, Spreadability, Triethanolamine, FTIR Spectroscopy, In vitro drug release, Absorption Maxima, Phosphate buffer solution, Extrudability, Penetration enhancer, Phyto-chemical tests, Viscosity of formulation.