Formulation and evaluation of mucoadhesive buccal tablets of nitrendipine
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and evaluation of mucoadhesive buccal tablets of nitrendipine
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.
This page presents a generated summary with additional references; See source (below) for actual content.
Original source:
This page is merely a summary which is automatically generated hence you should visit the source to read the original article which includes the author, publication date, notes and references.
Nayala Firdous and R. Balaji Reddy
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation and evaluation of mucoadhesive buccal tablets of nitrendipine
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Download the PDF file of the original publication
Summary of article contents:
Introduction
Mucoadhesive buccal tablets offer a promising alternative for drug delivery by allowing direct absorption through the buccal mucosa, which ensures rapid entry into systemic circulation. This study focuses on the formulation and evaluation of mucoadhesive buccal tablets of Nitrendipine, a calcium channel blocker, using various mucoadhesive polymers. The primary goal was to enhance the drug's bioavailability while minimizing the limitations associated with conventional oral administration, such as presystemic clearance in the liver.
Drug Release Kinetics
The dissolution studies conducted on the formulated buccal tablets revealed that formulations containing Acritamer 940 retarded drug release beyond eight hours, which was undesirable. In contrast, formulations F1, F7, and F8, which incorporated Manugel and Gum Cyamopsis, provided a satisfactory drug release profile, with F1 achieving the highest release of 96.35% by the end of eight hours. Kinetic analysis indicated that the drug release from the F1 formulation followed a non-Fickian diffusion mechanism, approximating zero-order kinetics. This finding emphasizes the formulation’s capability to maintain consistent drug delivery over an extended period.
Bioadhesion and Swelling Properties
Bioadhesion strength is a critical parameter for mucoadhesive systems, as it influences the retention of the dosage form in the oral cavity. The selected formulations exhibited satisfactory bioadhesive properties, with F1 demonstrating a peak detachment force of 16.43 N. Additionally, swelling studies were performed to assess how the mucoadhesive tablets interacted with the surrounding fluid, with F1 achieving a high swelling index over time. These results suggest that the formulation's design allows effective interaction with the mucosal environment, enhancing drug absorption.
Ex Vivo Permeation Studies
Ex vivo permeation studies through porcine buccal mucosa further validated the effectiveness of the optimized formulations. Among the selected formulations, F1 exhibited the highest flux value of 499.43 µg.hr⁻¹.cm⁻² and a significant permeability coefficient of 0.4994 cm/hr. These results imply that F1 effectively facilitates the transport of Nitrendipine across the buccal membrane, reinforcing its potential for clinical applications and highlighting its advantages over traditional oral delivery methods.
Conclusion
The study confirmed that the optimized F1 formulation of mucoadhesive buccal tablets containing 10 mg of Manugel exhibited exceptional bioadhesive properties, significant drug permeation, and favorable release kinetics. The long-term stability studies indicated that the formulation remained stable without significant changes in drug release, content, or bioadhesion over three months under controlled conditions. This highlights the potential of mucoadhesive buccal tablets as an effective delivery system for Nitrendipine, paving the way for improved therapeutic outcomes.
FAQ section (important questions/answers):
What is the purpose of Nitrendipine mucoadhesive buccal tablets?
The aim is to develop mucoadhesive buccal tablets of Nitrendipine, a calcium channel blocker, which allows drugs to enter the systemic circulation quickly through the buccal route.
What methods were used to formulate the buccal tablets?
The mucoadhesive buccal tablets were formulated using direct compression with polymers such as Manugel, Acretamer 940, and Gum Cyamopsis in various ratios.
How well did the formulations perform in drug release tests?
Formulations F1, F7, and F8 demonstrated optimal drug release rates of approximately 96.35%, 95.31%, and 93.48% respectively within 8 hours.
What stability conditions were the optimized formulations subjected to?
Short-term stability studies were conducted at 40±2ºC and 75±5% relative humidity over three months, showing no significant changes in drug release or content.
What were the results of the bioadhesion strength tests?
The selected formulations showed good bioadhesion strength, with F1 showing a peak detachment force of 16.43 N, indicating strong adhesion properties.
What kinetics did the optimized formulation follow during the release study?
The optimized formulation followed non-Fickian release kinetics, with characteristics approaching zero-order kinetics and a high regression value of 0.990.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Formulation and evaluation of mucoadhesive buccal tablets of nitrendipine”. 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:
In the context of pharmaceutical research, 'Drug' refers to the active ingredient being studied or formulated. Here, Nitrendipine is analyzed for its efficacy and delivery through mucoadhesive buccal tablets. The properties of the drug such as absorption, distribution, metabolism, and excretion are crucial in understanding its functionality and therapeutic effects.
2) Table:
The term 'Table' is significant in the realm of dosage forms, referring to tablets designed for drug delivery. The study focuses on buccal tablets, which utilize mucoadhesive properties to enhance bioavailability. Tablets are typically evaluated for their physical and chemical parameters, including hardness, friability, and drug release characteristics.
3) Swelling:
In this study, 'Swelling' pertains to the capacity of the mucoadhesive buccal tablets to absorb liquid and expand. Swelling is critical for assessing the tablets' ability to maintain contact with the mucosa, affecting drug release and bioadhesion. It’s an essential factor in understanding their performance in drug delivery systems.
4) Discussion:
The 'Discussion' section addresses the analysis and interpretation of experimental results obtained from the study. It provides insights into the performance of the formulations, including their drug release patterns, stability, and favorable properties. The discussion allows researchers to draw conclusions and suggest future research directions.
5) Channel:
'Channel' in this context refers to calcium channel blockers, such as Nitrendipine, which work by inhibiting calcium influx through cell membranes. Understanding the mechanism of action of such channels is vital in pharmacology and for developing effective therapeutic agents for conditions like hypertension.
6) Study (Studying):
The term 'Study' indicates systematic research aimed at investigating a specific hypothesis or question. In this article, the study involves the formulation and evaluation of mucoadhesive buccal tablets for Nitrendipine. The research encompasses various tests to determine the viability and effectiveness of the proposed drug delivery method.
7) Detachment:
'Detachment' refers to the process of the mucoadhesive tablet separating from the buccal mucosa. This characteristic is crucial for determining the bioadhesion strength of the tablet. Understanding how well a formulation adheres to the mucosal surface impacts its effectiveness in drug delivery systems.
8) Surface:
'Surface' pertains to the outer layer or area of the buccal tablets and the buccal mucosa they contact. The surface properties, including roughness and area, can significantly influence mucoadhesion and drug release characteristics, impacting overall therapeutic efficacy and patient compliance.
9) Pur (Pūr):
The term 'Poor' is used to describe unfavorable properties of certain formulations regarding flow or mechanical strength. Formulations labeled as 'poor' are less desirable for pharmaceutical preparations as they may lead to inconsistent or suboptimal drug delivery and could affect bioavailability.
10) Medium:
'Medium' refers to the solvent or dissolution environment in which the buccal tablets are tested, usually a buffer solution, like pH 6.8 phosphate buffer in this study. The medium's properties can affect drug release rates and bioavailability, critical in evaluating tablet performance.
11) India:
'India' indicates the geographical context where the study was conducted, providing relevance in terms of local pharmaceutical advancements, regulatory conditions, and traditional practices in drug formulation. The inclusion showcases regional contributions to global pharmaceutical research.
12) Water:
'Water' is critical in the swelling studies and drug release assessments of buccal tablets. It serves as a solvent and medium facilitating the absorption of the active ingredient and swelling of the tablets, impacting bioadhesion properties and overall drug delivery efficacy.
13) Blood:
'Blood' is indirectly referenced as the systemic circulation where the drug is intended to exert its therapeutic effects. Understanding how the drug enters the bloodstream after buccal administration is key to evaluating its pharmacokinetics and overall efficacy in treatment.
14) Post:
'Post' generally refers to subsequent evaluations conducted after the formulation processes, such as post-compression parameters. These evaluations are crucial for ensuring that the formulated buccal tablets meet required standards for physical and chemical properties necessary for effective drug delivery.
15) Activity:
'Activity' refers to the biological effectiveness of the drug, such as its pharmacological properties. In this study, the activity of Nitrendipine as an antihypertensive agent is examined, emphasizing the importance of delivering the drug effectively to achieve desired therapeutic outcomes.
16) Relative:
'Relative' typically pertains to comparative analyses within the study, especially concerning drug release or bioadhesion properties of different formulations. It helps in understanding how certain formulations perform in relation to each other and the implications for clinical effectiveness.
17) Heating:
'Heating' relates to the differential scanning calorimetry (DSC) used to study the thermal characteristics of the formulations. This technique helps reveal information about the physical and chemical stability of the drug-excipient mixtures, influencing the formulation processes employed.
18) Balaji:
'Balaji' refers to one of the authors of the study. Recognizing contributors is essential in scientific literature as it highlights the collaborative effort in research and development, attributing credit to individuals involved in the innovation of pharmaceutical formulations.
19) Powder:
'Powder' denotes the physical state of the formulation ingredients before compression into tablets. The properties of powder blend affect flow, compressibility, and ultimately the quality of the final tablet, making powder characteristics a crucial factor in dosage form development.
20) Filling (Filled):
'Filled' typically refers to how tablets are loaded with the active pharmaceutical ingredient and excipients. In this study, 'filled' tablets indicate proper formulation and manufacture, ensuring uniformity and consistency in drug delivery systems for optimal therapeutic efficacy.
21) Glass:
'Glass' in this study context refers to a type of apparatus used during experiments, such as dissolution testing. The use of glass slides allows for clear visibility and ease of handling during experimental procedures, ensuring accurate measurements and observations.