"Preparation and in-vitro study of nebivolol transdermal patches"

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Journal name: World Journal of Pharmaceutical Research
Original article title: Preparation and in-vitro characterization of nebivolol transdermal patches using solvent casting technique
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.

Summary of article contents:

Introduction

The research focuses on the development and evaluation of transdermal patches for the drug nebivolol, a cardioselective β1-receptor blocker used in hypertension treatment. The study highlights the advantages of transdermal delivery, including avoidance of first-pass metabolism and enhanced patient compliance, while addressing the challenges of drug permeation through the skin barrier.

Transdermal Patch Preparation and Evaluation

Transdermal patches of nebivolol were prepared using the solvent casting technique, utilizing various polymer combinations. The formulations were designed with different ratios of hydroxypropyl methylcellulose (HPMC K100, HPMC K4M), Metalose SR, along with additives like glycerin, Tween 80 as a penetration enhancer, and propylene glycol as a plasticizer. Twelve formulations were evaluated for physical and chemical properties, including thickness, drug content, moisture uptake, and mechanical strength.

Release Profile and Skin Permeation

The study revealed that the formulation containing HPMC K4M and HPMC K100 in a 1:4 ratio (F10) achieved the highest drug release (98.08% in 12 hours) and significant skin permeation rates (13.93 mg/cm²/h). This indicates that specific combinations of polymers can enhance the transdermal release and absorption of nebivolol effectively.

Stability and Interaction Studies

Fourier Transform Infrared (FTIR) spectroscopy was utilized to examine potential interactions between nebivolol and the polymers, confirming no significant chemical interaction that would affect drug stability. The stability studies demonstrated that the formulations maintained their physical and chemical properties over a period of 60 days under ambient conditions, indicating good stability for the transdermal patches.

Conclusion

The research successfully formulated matrix-type transdermal patches of nebivolol with favorable mechanical properties and drug release profiles. These patches are suitable for sustained and controlled drug delivery. Future work is encouraged to investigate their efficacy and bioavailability in clinical settings, along with further pharmacokinetic and pharmacodynamic evaluation.

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.

Author:

Jyothirmai.K , sonia. Sk, Lakshmana murthy.G, suchitra.M, venkata swathikrishna.K3, Krantikumar.P


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Preparation and in-vitro characterization of nebivolol transdermal patches using solvent casting technique

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


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FAQ section (important questions/answers):

What was the aim of the study on nebivolol transdermal patches?

The study aimed to develop and evaluate transdermal patches of nebivolol using the solvent casting technique, focusing on their in vitro drug release and mechanical properties.

What materials were used to prepare the transdermal patches?

The transdermal patches were prepared using polymers such as HPMC K100M, HPMC K4M, and Metalose SR, along with Tween 80 as a penetration enhancer and propylene glycol as a plasticizer.

What properties were evaluated for the prepared transdermal patches?

The patches were evaluated for thickness, mass variation, drug content, moisture uptake, tensile strength, folding endurance, and in vitro drug release studies to determine their suitability.

What was the maximum drug release percentage observed in the study?

The maximum drug release observed was 98.08% for formulation F10 over a 12-hour period, indicating effective drug release characteristics of the patch.

Did FTIR studies indicate interaction between nebivolol and the polymers?

FTIR studies showed no evidence of interaction between nebivolol and the polymers, suggesting compatibility in the formulation of the transdermal patches.

What conclusion was drawn from the study on nebivolol transdermal patches?

The study concluded that matrix-type transdermal systems for nebivolol could be effectively prepared, demonstrating suitable mechanical properties and controlled drug release for potential therapeutic applications.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “"Preparation and in-vitro study of nebivolol transdermal patches"”. 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 the active ingredient, nebivolol, investigated in this study. Nebivolol is a selective beta-blocker used in hypertension treatment, highlighting the article's focus on developing a transdermal delivery system that enhances its bioavailability and minimizes the first-pass metabolism typically seen in oral administration.

2) Table:
'Table' indicates the organized presentation of data, particularly regarding the formulations and evaluations of the transdermal patches. Tables summarize critical information like drug content, thickness, and in-vitro release studies, allowing for easier comparison between different formulations, crucial for drawing conclusions from the experiments.

3) Study (Studying):
'Study' denotes the scientific investigation into the development of nebivolol transdermal patches. The study encompasses the preparation, characterization, and evaluation of various patch formulations, emphasizing systematic experimentation and analysis to provide evidence-based conclusions about the effectiveness and properties of the drug delivery system.

4) India:
'India' signifies the geographical context in which the research was conducted. The article mentions specific institutions located in India, and the local educational environment might influence the methodology, availability of materials, and regulatory standards that pertain to pharmaceutical research within the country.

5) Transmission:
'Transmission' refers to the transfer of drug molecules through the skin (permeation), critical to transdermal systems. The study evaluates characteristics affecting drug transmission, including the formulation's composition and physical properties, thereby determining how effectively the nebivolol can permeate through the skin barrier.

6) Water:
'Water' is frequently involved in the preparation and evaluation processes in pharmaceutical formulations. It serves as a solvent or medium for various components, and understanding water's role, particularly in moisture content calculations, swelling index assessments, and vapor transmission studies, is imperative for optimizing formulations.

7) Measurement:
'Measurement' involves quantifying specific parameters of the transdermal patches, such as thickness, folding endurance, and weight. Accurate measurements are essential for assessing the quality and performance of each formulation, which directly impacts drug release rates, mechanical properties, and overall efficacy of the transdermal delivery system.

8) Discussion:
'Discussion' refers to the section where the authors interpret their findings, relating the results to other literature and hypotheses. It provides a platform for critical analysis of the implications of the study, allowing researchers to provide insights into the effectiveness of the transdermal patches and their potential clinical applications.

9) Swelling:
'Swelling' pertains to the change in volume or size of the transdermal patches upon reaching hydration equilibrium. Monitoring swelling behavior is crucial in assessing the patches' ability to perform effectively in vivo as it affects drug release kinetics and permeation profiles through the skin.

10) Nature:
'Nature' refers to the intrinsic characteristics of materials used in the transdermal patches and their interactions. Understanding the nature of the polymers and their role in controlling drug release and stability is essential in formulating effective drug delivery systems that cater to therapeutic demands.

11) Glass:
'Glass' generally refers to the use of glass vials or containers in experimental protocols, particularly for moisture vapor transmission studies. Its inertness and transparency make glass an ideal material for accurately measuring changes in weight or physical states of other substances, ensuring reliable results.

12) Biodegradable:
'Biodegradable' describes the polymers selected for the transdermal patches. The use of biodegradable materials suggests environmental and patient safety considerations, as these materials break down naturally and lessening the impact of disposal, thereby aligning the formulation with sustainable pharmaceutical practices.

13) Calculation:
'Calculation' refers to the quantitative analysis performed to interpret the results of various measurements conducted during the study. This could include determining drug release rates, permeability coefficients, or moisture content, which are vital for evaluating the patches' performance and effectiveness in drug delivery.

14) Observation:
'Observation' indicates the careful monitoring and recording of experimental results throughout the study. Detailed observations during tests such as drug release and mechanical property assessments are necessary to establish patterns and draw conclusions regarding the formulations' effectiveness and reliability.

15) Lakshmana (Lakṣmaṇa, Lakṣmaṇā):
'Lakshmana' is one of the authors of the study, representing contributors and their affiliations. Recognizing the authors lends credibility and potential for collaboration in further research initiatives, while also highlighting the academic effort behind the development of transdermal systems for drug delivery.

16) Substance:
'Substance' typically refers to the chemical components involved in the study. In this context, it includes nebivolol and various polymers used to create the transdermal patches, underscoring the importance of understanding each ingredient's role in achieving desired pharmacological effects.

17) Transformation (Transform, Transforming):
'Transform' entails the process of changing one state into another. The study's objective aimed to transform nebivolol from a conventional dosage form into a transdermal patch, improving therapeutic outcomes by enhancing bioavailability and allowing for a more controlled and sustained drug release.

18) Relative:
'Relative' often points to comparisons made between various formulations or their performance metrics. It indicates the importance of understanding how different formulations react in relation to one another, providing insights into which combinations yield optimal properties for effective drug delivery.

19) Sadhana (Sādhanā, Sādhana, Sadhāna):
'Sadhana' references the researcher's contribution within the study. By identifying their involvement, the work showcases collaborative efforts in pharmaceutical research, emphasizing the importance of academic contributions to the field's growth through joint investigations and development of drug delivery systems.

20) Venkata (Veṅkaṭa, Vemkata):
'Venkata' refers to another key contributing author in the investigation. Authorial recognition highlights the collaborative nature of the research and acknowledges contributions made in the development, experimentation, and evaluation of the transdermal delivery system for nebivolol.

21) Krishna (Kṛṣṇā, Kṛṣṇa):
'Krishna' is one of the authors mentioned in the research. Including author identities emphasizes the diversity of expertise and collaborative efforts in the study’s design and execution, contributing to the credibility of the findings related to transdermal drug delivery systems.

22) Chennai:
'Chennai' indicates the city associated with the institution providing the nebivolol sample. Recognizing the source underlines geographic implications of research and potential impact of local pharmaceutical initiatives, enhancing the context of the study within the broader scope of Indian pharmaceutical advancements.

23) Pouring:
'Pouring' describes an essential step in the solvent casting method used to prepare the transdermal patches. This process entails introducing polymer solutions into molds, which is crucial for shaping the patches and ensuring uniform distribution of the drug within the film matrix.

24) Surface:
'Surface' refers to the exposed area of the transdermal patches, which is significant for parameters like moisture transmission and drug permeation. The surface characteristics influence the drug's ability to diffuse across the skin barrier, making it a critical factor in transdermal patch design.

25) Powder:
'Powder' typically relates to the solid form of nebivolol employed in the transdermal formulations. The powder's physicochemical properties, including solubility and particle size, affect its formulation behavior and overall efficacy in the transdermal delivery system.

26) Dealer:
'Dealer' refers to the authorized source or supplier of chemical reagents and materials used in the study. Utilizing reliable dealers not only guarantees the quality of the substances but also ensures compliance with the necessary standards and regulations in pharmaceutical research.

27) Filling (Filled):
'Filled' denotes the action of incorporating components into specific configurations. In the context of the study, it typically refers to the process of adding drug-containing solutions into prepared molds before drying, forming the structure of the transdermal patches crucial for effective drug delivery.

28) Life:
'Life' in a pharmaceutical sense often pertains to the stability and shelf-life of the formulations being studied. Understanding a patch's life involves assessing how long it retains its efficacy and mechanical properties, which is vital for ensuring effective patient use and safety.

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