Optimizing norfloxacin nanoparticle gel for ocular drug delivery.
Journal name: World Journal of Pharmaceutical Research
Original article title: Optimization of 32 full factorial design based norfloxacin nanoparticles embedded thermo sensitive droppable gel for ocular drug delivery
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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Senthil Kumar Kannan, Dhachinamoorthi Duraisamy and Yajaman Sudhakar
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Optimization of 32 full factorial design based norfloxacin nanoparticles embedded thermo sensitive droppable gel for ocular drug delivery
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr201710-10729
Download the PDF file of the original publication
Summary of article contents:
Introduction
The study aimed to optimize and develop a nanoparticle-loaded thermo-sensitive droppable gel containing norfloxacin (NFLX) for ocular drug delivery, thereby enhancing bioavailability while addressing the limitations of conventional eye drops. Norfloxacin is a fluoroquinolone antibacterial agent often used in the treatment of bacterial conjunctivitis. However, traditional formulations are hindered by poor ocular bioavailability, frequent dosing, and rapid precorneal elimination. The proposed delivery system combines polymeric nanoparticles with thermo-sensitive gels, intending to create a formulation that provides controlled and prolonged drug release upon administration.
Optimization of Nanoparticle-Loaded Gel
An essential aspect of the research involved the optimization of the formulation using a 3² full factorial design. The design evaluated the effects of two independent variables, namely Pluronic-F-127 and HPMC K-100-M, on various response variables including gelation temperature, bioadhesive force, viscosity under physiological conditions, and cumulative drug release. Through the use of Design Expert software, polynomial equations were generated that described the relationships between these variables. The obtained results illustrated the potential for finer formulations with beneficial physical properties that correlate with enhanced ocular drug delivery.
Characteristics of the Developed Gel
The prepared nanoparticle-loaded thermo-sensitive droppable gel showed promising characteristics necessary for effective ocular application. The gel demonstrated a gelation temperature appropriate for physiological conditions, allowing it to transition from a liquid to a gel state upon coming into contact with tear fluid in the eye. The drug content was acceptable, and the formulation retained a stable pH of around 7.4, ensuring compatibility with ocular tissues. Evaluation of the gel's physical properties revealed that it exhibited shear-thinning behavior, improving patient comfort and delivery during blinking, an important factor for successful ocular treatment.
Drug Release and Antibacterial Efficacy
The in vitro drug release studies indicated that the formulation could sustain the release of NFLX over an extended period, significantly longer than traditional eye drop formulations. The kinetic analysis suggested that drug release follows a non-Fickian diffusion mechanism, wherein both swelling and erosion of the polymer matrix occur. Additionally, antibacterial studies revealed that the optimized formulation exhibited enhanced bactericidal activity against common ocular pathogens like Pseudomonas aeruginosa and Staphylococcus aureus, highlighting its potential as a superior alternative to existing treatment options.
Conclusion
This study successfully developed a nanoparticle-based thermo-sensitive droppable gel for ocular drug delivery, demonstrating prolonged drug release, favorable biocompatibility, and effective antibacterial action. The formulation addresses the limitations associated with conventional eye drops and holds promise for improving patient compliance due to its ease of administration and reduced dosing frequency. Future research may further elucidate the long-term efficacy and safety of this innovative delivery system in clinical settings, making it a viable option for treating eye infections.
FAQ section (important questions/answers):
What was the objective of the study on norfloxacin nanoparticles?
The study aimed to fabricate and optimize a nanoparticle-loaded thermo-sensitive droppable gel for ocular drug delivery of norfloxacin to enhance bioavailability and reduce frequent dosing.
What method was used to prepare norfloxacin nanoparticles?
Norfloxacin nanoparticles were prepared by the nanoprecipitation method, followed by characterization for particle size, zeta potential, and drug entrapment efficiency.
What factors were optimized in the formulation design?
The study utilized a 3² full factorial design to evaluate the effects of Pluronic-F-127 and HPMC K-100-M on gel properties like gelation temperature and bioadhesive strength.
How did the optimized formulation perform in drug release studies?
The optimized NP-TDGL formulation demonstrated cumulative drug release between 57.67% to 85.61% over six hours, indicating controlled release characteristics.
What were the findings regarding ocular irritation from the formulation?
The optimized formulation showed no signs of eye irritation in both the HET-CAM test and the in vivo irritation study with New Zealand White rabbits.
What advantages does the NP-TDGL formulation offer for ocular delivery?
The NP-TDGL formulation provides prolonged corneal residence time, improved bioavailability, and potential reduction in dosing frequency compared to conventional eye drops.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Optimizing norfloxacin nanoparticle gel for ocular drug delivery.”. 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 substance used to diagnose, cure, treat, or prevent disease or enhance physical or mental well-being. In the context of this study, Norfloxacin is the active pharmaceutical ingredient being formulated into nanoparticles for ocular delivery, highlighting its importance in pharmaceutical research and therapy.
2) Table:
In scientific research, tables are used to organize and present data clearly and succinctly. This study includes various tables to illustrate experimental designs, formulations, and results, making it easier for readers to understand the research findings, compare variables, and analyze outcomes effectively.
3) Medium:
A medium in this context refers to a substance or environment for biological or chemical reactions. The study involves artificial tear fluid as the medium for in-vitro drug release testing, mimicking physiological conditions for realistic assessment of the drug's behavior in the eye.
4) Study (Studying):
A study is a detailed examination and analysis of a subject. This research focuses on developing and optimizing a nanoparticle-loaded thermo-sensitive gel for drug delivery. The study's structured approach, including experimentation and evaluation, contributes to advancements in ocular drug formulation technology.
5) Water:
Water is a solvent commonly used in pharmaceutical formulations. It is essential for dissolving active ingredients and excipients in the preparation of nanoparticles and gels. The purity and quality of water in experiments can significantly impact the formulation’s performance and stability.
6) Surface:
Surface refers to the outermost layer or boundary of a substance. In this study, the surface characteristics of nanoparticles are crucial as they influence drug release rates, interaction with ocular tissues, and overall bioadhesive properties, impacting the effectiveness of ocular delivery systems.
7) Measurement:
Measurement is the process of determining the size, quantity, or degree of something. In this research, various measurements, such as viscosity, particle size, and drug release, are performed to ensure that the formulations meet the desired criteria for efficacy, safety, and stability in ocular applications.
8) India:
India is the country where this research originates. The pharmaceutical landscape in India plays a significant role in global drug production, and studies like this contribute to advancements in drug delivery systems, especially in addressing local healthcare needs and enhancing therapeutic options.
9) Irritation:
Irritation refers to a sensation of discomfort or adverse reaction caused by certain substances. Assessing ocular irritation from formulations is critical in this study to ensure safety and comfort for patients, guiding the formulation development towards non-irritating products suitable for eye use.
10) Swelling:
Swelling signifies the increase in size or volume due to absorption or inflammation. In ocular formulations, swelling behavior of gels is important as it affects the release and retention of the drug in the eye, impacting therapeutic effectiveness and patient comfort.
11) Tear:
Tears are physiological fluids produced by the body to lubricate and protect the eyes. In this study, artificial tear fluid is used to simulate the ocular environment for evaluating formulation behavior, ensuring relevance to real-life conditions and enhancing the drug delivery's effectiveness.
12) Andhra (Amdhra):
Andhra refers to Andhra Pradesh, the Indian state where the research was conducted. This region is home to several pharmaceutical institutions and industries, contributing to the development of innovative drug delivery systems and enhancing public health through local research initiatives.
13) Blood:
Blood is a vital fluid that transports oxygen and nutrients throughout the body. In the context of this research, blood may be referenced during isotonicity tests to ensure that formulations do not adversely affect cellular integrity, highlighting the importance of biocompatibility in ocular drug delivery.
14) Hand:
Hand refers to the human appendage used for manual tasks. In the study's context, handshaking may be referenced during the preparation stages of formulations, emphasizing the importance of consistent techniques to ensure uniformity and reproducibility in nanoparticle dispersion and gel preparation.
15) Antibiotic (Antibacterial):
Antibacterial denotes substances that prevent the growth of bacteria. Norfloxacin, the drug studied here, has antibacterial properties that are critical for treating ocular infections. The study evaluates its delivery via novel formulations to optimize therapeutic efficacy and combat bacterial resistance.
16) Glass:
Glass is a transparent, hard material commonly used in laboratory equipment. In this study, glass containers may be used for storing formulations and conducting experiments. The use of glass minimizes contamination and preserves the integrity of the formulations being studied.
17) Sign:
Sign refers to an observable indication or evidence of a phenomenon. In this research, signs of drug release, bioadhesion, or irritation are critically analyzed, helping to deduce the effectiveness of the developed formulations in treating ocular conditions.
18) Transmission:
Transmission refers to the act of conveying or passing through. In the context of this study, transmission techniques such as electron microscopy may be used to examine nanoparticles, ensuring that their characteristics and behaviors are accurately assessed for ocular delivery applications.
19) Detachment:
Detachment refers to the process of separating or removing something. In this study, detachment is measured to evaluate the bioadhesive properties of formulations. Understanding how well gels stay adhered to ocular surfaces informs their potential effectiveness in drug delivery.
20) Container:
Container refers to an object that holds or transports substances. In pharmaceutical research, the choice of container can influence the stability and integrity of formulations. Properly sealed and sterile containers are essential for preserving the quality of developed drug delivery systems.
21) Science (Scientific):
Science is the systematic study of the natural world through observation and experimentation. This study exemplifies scientific inquiry in pharmaceutical science, emphasizing the importance of research methodologies in developing safer and more effective drug delivery systems for ocular applications.
22) Kannan:
Kannan likely refers to one of the authors of the study, specifically Senthil Kumar Kannan. His contributions to the research and findings presented demonstrate the collaborative effort in advancing pharmaceutical formulations and addressing ocular drug delivery challenges.
23) Nature:
Nature encompasses the physical world and its inherent qualities. The study takes into account natural properties of polymers and nanoparticles to formulate effective drug delivery systems, reflecting the interplay between synthetic ingredients and biological interactions for therapeutic use.
24) Indian:
Indian refers to aspects related to India, including cultural, geographical, and scientific contexts. This study contributes to the body of pharmaceutical research being conducted in India, focusing on developing innovative drug delivery mechanisms to address local healthcare demands.
25) Kumar:
Kumar is a common surname in India, and in this context, it could refer to Senthil Kumar Kannan, emphasizing collaborative research. His role in the study highlights the contributions of individual researchers towards advancements in the field of pharmaceutical sciences.
26) Pur:
Poor describes inadequate or unsatisfactory conditions. In this study, Norfloxacin is characterized as a poorly soluble drug, which presents challenges for effective ocular delivery. The research aims to improve drug formulation to enhance solubility and bioavailability for therapeutic use.
27) Performance:
Performance refers to how effectively a formulation achieves its intended purpose. This study assesses the performance of the developed nanoparticle-loaded gel in terms of drug release and biocompatibility, guiding improvements in ocular drug delivery technology.
28) Observation:
Observation denotes the act of monitoring and recording data during experiments. This study relies heavily on observations during formulation tests to evaluate characteristics such as viscosity, bioadhesion, and drug release, ensuring accurate results and informed conclusions.
29) Discussion:
Discussion is a section where research findings are interpreted and contextualized. In this study, the discussion reflects on the significance of results, their implications for ocular drug delivery, and how the study contributes to existing knowledge in pharmaceutical sciences.
30) Substance:
Substance refers to a material with distinct physical properties. In this research, various substances, including polymers and drugs, are studied to understand their interactions and contributions to the overall effectiveness and stability of ocular delivery formulations.
31) Observing:
Observing involves careful monitoring of phenomena or experiments. In this study, researchers are observing the effects of formulation components on drug release and bioadhesion, ensuring that the developed systems are effective and safe for ocular application.
32) Activity:
Activity refers to the observable behavior or function of a substance or system. In the study, the antibacterial activity of Norfloxacin against specific bacteria is assessed, highlighting the significance of formulation design in enhancing therapeutic efficacy.
33) Lighting:
Lighting refers to light conditions in an environment. While not directly related to the study, appropriate lighting may be important for accurate observations and measurements during experiments, ensuring that visual assessments of formulations are clear and reliable.
34) Relative:
Relative helps to compare one element to another. In this study, the performance of new formulations is evaluated relative to existing treatments, highlighting advancements in ocular drug delivery systems and their effectiveness compared to conventional methods.
35) Chennai:
Chennai is a major city in India, known for its contributions to education and research. It represents a location for potential collaboration or sourcing of materials in the pharmaceutical field, relevant to the context of Indian pharmaceutical advancements.
36) Methane:
Methane is a simple hydrocarbon gas. In this study, it may reference solvents used during the formulation process; however, it is imperative that any solvent used is safe and appropriate for pharmaceutical applications, ensuring effective and stable formulations.
37) Aureus:
Aureus refers to Staphylococcus aureus, a significant bacterial pathogen. This study examines the efficacy of Norfloxacin-loaded formulations against this bacterium, emphasizing the importance of effective antibacterial treatments for ocular infections and the formulation's clinical relevance.
38) Filling (Filled):
Filled refers to the act of completing a container with a substance. In pharmaceutical terms, it may indicate how formulations are prepared or packaged, pertaining to quality control in ensuring that dosage forms are adequately filled for accurate dosing.
39) Kadapa:
Kadapa is a city in Andhra Pradesh, India. In the context of this study, it could indicate the geographical location of research or collaboration, contributing to the research environment in the region and supporting local advancements in pharmaceutical studies.
40) Edema (Oedema):
Edema refers to swelling caused by fluid accumulation. In ocular contexts, this could indicate a condition targeted by the developed therapeutic formulation. Assessing the formulation's ability to alleviate edema reflects its potential therapeutic applications.
41) Death:
Death refers to the cessation of life. In the study, while it may not directly apply, it underscores the seriousness of bacterial infections like conjunctivitis and the need for effective treatments that can prevent complications, thus reinforcing the importance of innovative formulations.
42) Soya:
Soya often references soybean-derived components. In pharmaceutical formulations, soy products like lecithin could serve as emulsifiers or stabilizers, emphasizing the study’s exploration of natural substances in enhancing the effectiveness and safety of ocular drug delivery systems.
43) Gold (Golden):
Gold can refer to an element often used in scientific applications, including nanoparticle synthesis and characterization. Its reference in this study might highlight advanced methodologies employing gold nanoparticles for enhanced drug delivery systems, signaling innovations in ocular therapeutics.