A Review on Polymer as Multifunctional Excipient in Drug Delivery System
Dushing Kiran R, Siddheshwar S S
Pravara Rural College of Pharmacy, Pravaranagar A/P Loni, 413736, Tal – Rahata, Dist. – Ahmednagar.
*Corresponding Author E-mail: krndushing@gmail.com
ABSTRACT:
Polymer-based drug delivery systems have gained significant attention in the field of pharmaceutical research due to their multifunctional nature. These systems utilize various polymers to encapsulate and deliver therapeutic agents, providing enhanced drug stability, controlled release, and targeted delivery to specific sites within the body. Here, we’ll discuss the multifunctionality of polymers in drug delivery systems and their potential applications.
KEYWORDS: Multifunctional Polymer, Polymer Excipient, Polymer Therapeutics, Tissue engineering, Bio imaging, Biosensor.
INTRODUCTION:
Polymers are large molecules composed of repeating subunits called monomers. They are formed through a process called polymerization, where monomers chemically bond together to form a long chain or network structure. The resulting polymer can have a wide range of properties depending on the choice of monomers and the polymerization process.1
Properties of polymers can vary significantly and are influenced by several factors, including the chemical structure of the monomers, the molecular weight of the polymer, the degree of polymerization, and the presence of any additives or fillers. Here are some common properties of polymers:1
1. Mechanical Properties: Polymers can exhibit a wide range of mechanical properties, from soft and flexible to hard and rigid. Some polymers are highly elastic and can stretch significantly before breaking, while others are more brittle and prone to fracture. 1
2. Molecular Weight: Polymers can have a range of molecular weights, from a few thousand to millions of atomic mass units. The molecular weight affects various properties, such as mechanical strength, viscosity, and thermal stability. 1
3. Processing Characteristics: Polymers can be processed using various techniques like extrusion, injection molding, blow molding, and casting. The processability of a polymer depends on factors such as melt viscosity, melt temperature, and the presence of any additives or fillers. 2
4. Thermal Properties: Polymers have different thermal characteristics, including melting point, glass transition temperature, and thermal conductivity. These properties determine how polymers behave under different temperature conditions and can influence their processing and applications.3
5. Chemical Resistance: Polymers can be resistant to various chemicals, including acids, bases, solvents, and oils. However, their resistance depends on the specific polymer composition and the nature of the chemical substances they come into contact with.4
It's important to note that the properties of specific polymers can differ significantly, and there are numerous types of polymers available with unique characteristics tailored for specific applications.
2. POLYMER IN BIOMEDICAL APPLICATION:
Multifunctional polymers play a significant role in various biomedical applications due to their unique properties and versatility. These polymers are designed to possess multiple functions or capabilities that can be tailored for specific applications in medicine and healthcare. Here are some examples of how multifunctional polymers are used in biomedical applications:
Fig: Biomedical Applications of Polymers
1. Drug Delivery Systems: Multifunctional polymers are extensively used in designing drug delivery systems. These polymers can encapsulate drugs or therapeutic agents and release them at a controlled rate, improving drug efficacy and reducing side effects. They can be designed to respond to various stimuli such as pH, temperature, or enzymatic activity, enabling targeted and site-specific drug delivery. Additionally, multifunctional polymers can be functionalized with targeting ligands to enhance the specificity of drug delivery to specific cells or tissues.5
2. Tissue Engineering: Multifunctional polymers are employed in tissue engineering to create scaffolds that mimic the extracellular matrix (ECM) and promote tissue regeneration. These polymers can provide mechanical support to cells and offer a biocompatible environment for their growth. They can be functionalized with bioactive molecules such as growth factors, peptides, or cell adhesion molecules to enhance cell attachment, proliferation, and differentiation. Moreover, multifunctional polymers can incorporate properties like biodegradability, porosity, and surface modifications to promote tissue regeneration.6
3. Bioimaging: Multifunctional polymers are utilized in various bioimaging techniques for diagnostic purposes. These polymers can be functionalized with imaging agents such as fluorescent dyes, quantum dots, or magnetic nanoparticles, enabling enhanced contrast and visualization of tissues or cells. Multifunctional polymers can also be engineered to target specific biomarkers, allowing for targeted imaging of diseases like cancer or cardiovascular disorders.7
4. Biosensors and Diagnostics: Multifunctional polymers are employed in biosensors and diagnostic platforms. They can serve as the matrix for immobilizing biomolecules like antibodies, enzymes, or DNA probes, enabling specific detection of target analytes. Multifunctional polymers can also provide signal amplification or signal transduction capabilities, improving the sensitivity and accuracy of diagnostic tests. Additionally, these polymers can be integrated into microfluidic devices, creating portable and point-of-care diagnostic tools.8
5. Antimicrobial Coatings: Multifunctional polymers can be utilized to develop antimicrobial coatings for medical devices, surfaces, or implants. These polymers can release antimicrobial agents to prevent the colonization of bacteria or fungi, reducing the risk of infections. They can also possess other functionalities such as biocompatibility, anti-inflammatory properties, or biofilm inhibition, making them suitable for a wide range of biomedical applications.9
Overall, multifunctional polymers offer tremendous potential in biomedical applications by providing tailored functionalities and enabling advancements in drug delivery, tissue engineering, bioimaging, diagnostics, and antimicrobial strategies. Ongoing research and development in this field continue to expand the capabilities and applications of multifunctional polymers in medicine and healthcare.
3. DIFFERENT USES OF POLYMER IN DIFFERENT DOSAGE FORMS:
Polymers are widely used in various dosage forms to enhance drug delivery, stability, and patient compliance. Here are some different uses of polymers in different dosage forms:
Tablets and Capsules:
· Binders: Polymers such as hydroxypropyl cellulose (HPC), hydroxypropyl methylcellulose (HPMC), and polyvinylpyrrolidone (PVP) are used as binders to hold the tablet ingredients together.
· Disintegrants: Polymers like croscarmellose sodium, crospovidone, and sodium starch glycolate are used as disintegrants to facilitate the breakup of tablets or capsules in the gastrointestinal tract, promoting drug dissolution and absorption.
· Extended-release formulations: Polymers such as ethyl cellulose, methyl cellulose, and polyvinyl alcohol (PVA) can be used to create sustained-release or controlled-release formulations, allowing for a prolonged drug release.
· Film Coating: Polymers are employed in film coating applications to provide a protective layer on tablets or capsules. Film coatings can improve the appearance, taste, and stability of the dosage form, as well as mask any unpleasant odors. Polymers used in film coating formulations may include hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol (PVA), polyethylene glycol (PEG), and methacrylic acid copolymers.
· Controlled-release matrices: Polymers can be used as matrix materials in controlled-release tablet formulations. They act as carriers for the drug, controlling its release rate over time. By altering the polymer composition and structure, drug release kinetics can be modified to achieve specific therapeutic objectives. Commonly used polymers in controlled-release matrices include hydroxypropyl methylcellulose (HPMC), polyethylene oxide (PEO), and ethyl cellulose.10
|
Functional Role |
Examples |
Description and functionality |
|
Filler |
· MCC |
· Add bulk to the dosage form. · May contribute to dissolution and disintegration characteristics. |
|
Binder |
· PVP · HPC · Starch |
· Bind the powder to form granule for processing. |
|
Disintegrant |
· Croscarmellose sodium · Crospovidone · Sodium starch glycolate · Starch |
· Disintegration of the tablet to granules and powder on coming in contact with water. |
|
Coating material |
· HPMC · Ethyl cellulose · Polyvinyl alcohol · Plasticizer ex. PEG |
· Provide a physical barrier coating on the surface of the compressed core tablet. |
Injectable Formulations:
· Stabilizers: Polymers like polyethylene glycol (PEG) and polyvinylpyrrolidone (PVP) are used as stabilizers to prevent aggregation or precipitation of drug molecules in injectable formulations.
· Hydrogels: Injectable hydrogels composed of polymers such as polyethylene glycol diacrylate (PEGDA), poly (lactic-co-glycolic acid) (PLGA), or poly(N-isopropylacrylamide) (PNIPAAm) are used for sustained drug release, tissue engineering, and local drug delivery.
· Microparticles/Nanoparticles: Polymers are used to encapsulate drugs or therapeutic agents within microparticles or nanoparticles for injectable formulations. These polymer-based drug delivery systems offer advantages such as improved drug stability, controlled release, and targeted delivery. Polymers like poly (lactic-co-glycolic acid) (PLGA), polyethylene glycol (PEG), and poly (lactic acid) (PLA) are commonly used in the preparation of injectable microparticles or nanoparticles.11
Topical Formulations:
Polymers play various roles in topical applications, providing desirable properties and functionalities to formulations. Here are some common uses of polymers in topical applications:
· Gelling agents: Polymers like carbomer, hydroxyethyl cellulose (HEC), and polyvinyl alcohol (PVA) are used as gelling agents in topical formulations, providing viscosity and spread ability.
· Mucoadhesive polymers: Polymers such as chitosan, polyvinylpyrrolidone (PVP), and hyaluronic acid can be used in topical formulations to improve adhesion to mucosal surfaces and enhance drug retention.
· Film Formers: Polymers can act as film formers in topical formulations, creating a protective layer on the skin surface. The film helps improve the stability of active ingredients, prevent moisture loss, and provide a barrier against external irritants. Polymers such as polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA), and polyethylene glycol (PEG) are commonly used as film formers.
· Emulsifiers and Stabilizers: Polymers are employed as emulsifiers and stabilizers in topical emulsion formulations. They help disperse immiscible components, such as oil and water, and prevent phase separation. Polymers like polysorbate 80, acrylates/C10-30 alkyl acrylate cross polymer, and cetyl alcohol are commonly used for emulsification and stabilization.
· Controlled Release Systems: Polymers are used in topical formulations to create controlled release systems, allowing for sustained drug release over a prolonged period. These polymers can control the release rate of active ingredients, prolong their therapeutic effects, and reduce the frequency of application. Examples of polymers used in controlled release systems include ethyl cellulose, polyethylene glycol (PEG), and poly (lactic-co-glycolic acid) (PLGA).
· Rheology Modifiers: Polymers can function as rheology modifiers in topical formulations, controlling the viscosity and flow properties of the product. They ensure proper spread ability, ease of application, and desired texture. Common rheology modifiers include xanthan gum, carbomers, and hydroxyethyl cellulose (HEC).12
Transdermal Patches:
Polymers play a crucial role in transdermal patches, which are designed to deliver drugs through the skin and into the bloodstream. Here are some common uses of polymers in transdermal patches:
· Drug matrix: Polymers like polyacrylate adhesives or silicone-based polymers are used as drug matrices in transdermal patches, providing controlled drug release through the skin.
· Permeation enhancers: Certain polymers, such as polyvinylpyrrolidone (PVP) or polyethylene glycol (PEG), can act as permeation enhancers to improve the absorption of drugs through the skin.
· Adhesive Matrix: Polymers serve as adhesive matrices in transdermal patches, allowing the patch to adhere to the skin while delivering the drug. The adhesive matrix not only ensures proper patch adhesion but also controls the drug release through the skin. Common adhesive polymers used in transdermal patches include acrylic adhesives, silicone-based polymers, and polyisobutylene.
· Backing Film: Polymers are used to create the backing film of transdermal patches, which provides structural support and protects the drug reservoir and adhesive layer. The backing film should be impermeable to the drug and moisture, maintaining the integrity of the patch. Common polymer materials used for backing films include polyester (PET), polyethylene terephthalate (PET), and polyurethane.
· Protective Overlays/Liners: Polymers can be used as protective overlays or liners in transdermal patches to protect the drug reservoir and adhesive layers during manufacturing, storage, and application. These overlays prevent drug loss, maintain patch integrity, and provide a barrier against external contaminants. Common polymer materials used as protective overlays include silicone-coated polyester films and polyethylene films.13
Inhalation Formulations:
Polymers have several important uses in inhalation formulations, which are designed to deliver drugs directly to the respiratory system. Here are some common uses of polymers in inhalation formulations:
· Excipients for dry powder inhalers: Polymers like lactose, mannitol, and glucose are used as carrier particles for dry powder inhalers, facilitating the dispersion and delivery of drug particles to the lungs.
· Aerosol propellants: Certain polymers, such as hydrofluoroalkanes (HFAs), are used as propellants in metered-dose inhalers (MDIs) to deliver drugs in aerosol form.
· Excipients for Inhalation Solutions and Suspensions: Polymers are employed as excipients in inhalation solutions and suspensions to improve their stability, enhance drug solubility, and control the rate of drug release. These polymers can assist in maintaining the formulation integrity, preventing particle aggregation, and ensuring homogeneity. Commonly used polymers include hydroxypropyl cellulose (HPC), polyvinyl alcohol (PVA), and polyethylene glycol (PEG).
· Particle Coating: Polymers are used for coating drug particles in inhalation formulations. Coating the drug particles with a polymer layer can protect the drug from degradation, improve dispersibility, and control the release rate of the drug upon inhalation. The choice of polymer for particle coating depends on the specific drug and desired release profile. Examples of polymers used for particle coating in inhalation formulations include poly (lactic-co-glycolic acid) (PLGA), ethyl cellulose, and acrylic polymers.
· Nasal Spray Formulations: Polymers are used in nasal spray formulations to enhance drug delivery and retention in the nasal cavity. These polymers can improve drug solubility, viscosity, and muco adhesion. They assist in prolonging the contact time of the drug with the nasal mucosa, enhancing drug absorption. Examples of polymers used in nasal spray formulations include hydroxypropyl methylcellulose (HPMC), chitosan, and xanthan gum.
These are just a few examples of how polymers are utilized in different dosage forms. The selection of a specific polymer depends on factors such as drug characteristics, desired drug release profile, route of administration, stability requirements, and patient considerations. Different polymers offer unique properties and functionalities that can be tailored to meet the specific needs of each dosage form. 14
4. CONCLUSION:
In conclusion, polymers play a crucial role in drug delivery systems, offering numerous advantages and possibilities in the field of pharmaceutical sciences. The use of polymers allows for the development of controlled and targeted drug delivery systems, enhancing the efficacy and safety of therapeutic treatments.
Polymers provide a versatile platform for drug encapsulation and release, allowing for the protection and controlled release of drugs, thereby improving their bioavailability and reducing potential side effects. By altering the properties of the polymer matrix, such as its composition, molecular weight, and architecture, researchers can modulate the drug release kinetics to meet specific therapeutic requirements.
Polymeric drug delivery systems also offer advantages such as prolonged release profiles, improved stability, and protection of the drug from degradation, enhancing its shelf life and ensuring consistent therapeutic efficacy. Additionally, polymers can be tailored to respond to various stimuli, including pH, temperature, enzymes, or light, enabling site-specific and on-demand drug release in response to specific physiological conditions.
Furthermore, polymers used in drug delivery systems can be engineered to target specific tissues, cells, or organelles, improving drug concentration at the desired site while minimizing exposure to healthy tissues. This targeted delivery approach enhances the therapeutic index of drugs, reducing systemic toxicity and improving patient compliance.
The development of biodegradable and biocompatible polymers has also contributed to the advancement of drug delivery systems. These polymers can be safely administered, metabolized, and eliminated from the body, minimizing potential long-term adverse effects.
In summary, the use of polymers in drug delivery systems has revolutionized the field of pharmaceutical sciences, offering improved drug efficacy, safety, and patient outcomes. Continued research and innovation in polymer design and fabrication techniques hold great promise for the development of even more sophisticated and effective drug delivery systems in the future.
5. REFERENCE:
1. Deepak Sen et al, Int. Journal of Pharmaceutical Sciences and Medicine (IJPSM). 2019; 4(10): 1-15.
2. Müller K, Bugnicourt E, Latorre M, Jorda M, Echegoyen Sanz Y, Lagaron JM, Miesbauer O, Bianchin A, Hankin S, Bölz U, Pérez G, Jesdinszki M, Lindner M, Scheuerer Z, Castelló S, Schmid M. Review on the Processing and Properties of Polymer Nanocomposites and Nanocoatings and Their Applications in the Packaging, Automotive and Solar Energy Fields. Nanomaterials (Basel). 2017; 7(4): 74. doi: 10.3390/nano7040074. PMID: 28362331; PMCID: PMC5408166.
3. Short Review on Thermal and Mechanical Properties of Polymers, International Journal of Emerging Technologies and Innovative Research. 2019; 6(1): 247-250
4. Seymour, R. B., and Carraher, C. E. Structure—Property Relationships in Polymers. 1984. doi:10.1007/978-1-4684-4748-4.
5. Liechty WB, Kryscio DR, Slaughter BV, Peppas NA. Polymers for drug delivery systems. Annu Rev Chem Biomol Eng. 2010; 1: 149-73. doi: 10.1146/annurev-chembioeng-073009-100847. PMID: 22432577; PMCID: PMC3438887.
6. Trinath Biswal, Biopolymers for tissue engineering applications: A review, Materials Today: Proceedings. 2021; 41(2): 397-402 https://doi.org/10.1016/j.matpr.2020.09.628.
7. Kim, Jong Ho; Park, Kyeongsoon; Nam, Hae Yun et al. Polymers for bioimaging. In: Progress in Polymer Science (Oxford). 2007; 32(8-9): 1031-1053.
8. Davis, Frank and Séamus P. J. Higson. Polymers in Biosensors. 2007.
9. Sanjeeva, Sandesh and Bajire, Sukesh, P Shastry, Rajesh and Johnson, Renjith. Antimicrobial coatings based on polymeric materials. 2023. 10.1016/B978-0-323-99291-6.00015-3.
10. Debotton N, Dahan A. Applications of Polymers as Pharmaceutical Excipients in Solid Oral Dosage Forms. Med Res Rev. 2017; 37(1): 52-97. doi: 10.1002/med.21403. Epub 2016 Aug 9. PMID: 27502146.
11. Imran Vhora, Nirav Khatri, Ambikanandan Misra, Chapter 8 - Applications of Polymers in Parenteral Drug Delivery, Editor(s): Ambikanandan Misra, Aliasgar Shahiwala, Applications of Polymers in Drug Delivery (Second Edition), Elsevier, 2021; 221-261, ISBN 9780128196595,
12. Yadav K, Soni A, Singh D, Singh MR. Polymers in topical delivery of anti-psoriatic medications and other topical agents in overcoming the barriers of conventional treatment strategies. Prog Biomater. 2021; 10(1): 1-17. doi: 10.1007/s40204-021-00154-7. Epub 2021 Mar 18. PMID: 33738750; PMCID: PMC8021620.
13. Sabbagh F, Kim BS. Recent advances in polymeric transdermal drug delivery systems. J Control Release. 2022; 341:132-146. doi: 10.1016/j.jconrel.2021.11.025. Epub 2021 Nov 20. PMID: 34813879.
14. Al-Nemrawi, N.K., Darweesh, R.S., Al-shriem, L.A., Al-Qawasmi, F.S., Emran, S.O., Khafajah, A.S., and Abu-Dalo, M.A. (2022). Polymeric Nanoparticles for Inhaled Vaccines. Polymers. 14.
Received on 27.07.2023 Modified on 28.08.2023
Accepted on 18.09.2023 ©Asian Pharma Press All Right Reserved
Asian J. Res. Pharm. Sci. 2023; 13(4):325-329.
DOI: 10.52711/2231-5659.2023.00055