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Application of Polymers in the Pharmaceuticals

and Advantages of Polymers use in the Novel Drug


Delivery System

Name: M. Bilal
RollNo: 1163
Batch: 15th
Semester: 9th
Subject: Pharamaceutical Technology
Subject Incharge: Sir Asif

FACULTY OF PHARMACY
HAJVERY UNIVERSITY, LAHORE
Introduction

Polymeric drug delivery systems are achieved great development within the last 20 years . Polymeric
drug delivery has defined as a formulation or a tool that permits the introduction of a therapeutic
substance into the body. Biodegradable and bio-reducible polymers make the magic possible choice
for tons of latest drug delivery systems. the longer term prospects of the research for practical
applications has required for the event within the field.
The research for polymeric drug delivery has been progressed for an extended time since the 1980s.
The searches for brand spanking new drug delivery systems approaches and new modes of action
represent one among the frontier research areas. Those involve multi-disciplinary scientific
approaches to supply major advances in an improving therapeutic index and bioavailability at the
precise delivery of medicine. Drug delivery system combines one or more traditional drug delivery
systems with engineered technologies though. The systems create the power to specifically targeting
points where a drug has been released within the body and/or the speed at which it's been released.

Polymers play a serious role in drug delivery technology development by releasing two sorts of :
hydrophilicity and hydrophobic. During a synchronized manner and constant release of formulations
over extended periods though. There are numerous advantages of polymers acting as an inert carrier to
which a drug are often conjugated, for instance , the polymer improves the pharmacokinetic and
pharmacodynamic properties of biopharmaceuticals through various ways, like plasma ½ life,
decreases the immunogenicity, build-ups the steadiness of biopharmaceuticals, improves the solubility
of low relative molecular mass drugs, and features a potential of targeted drug delivery. However,
they need their own limitations, like the naturals polymers are most abundant and biodegradable but
are difficult to breed and purify. Synthetic polymers have high immunogenicity, which prevents their
long-term usage. Non-biodegradable polymers are needed to be sugary after they release the drug at
the targeted site. the overall characteristic features that make the polymer a possible candidate for
drug delivery include, safety, efficacy, hydrophilicity, absence of immunogenicity biological
inactivity, sufficient pharmacokinetics though, and presence of functional groups for covalent
conjugation of medicine , targeting moieties, or formation of the copolymer.

Polymers are substances whose molecules have high molar masses and are compressed by an
outsized number of repeating units. Polymers can form particles of solid dosage form and can also
change the flow property of liquid dosage form. Polymers are the backbone of pharmaceutical drug
delivery systems. Polymers are used as a crucial tool to regulate the drug release rate from the
formulation. they're also mostly used as stabilizers, taste-making agents, and proactive agents.
Modern advances in drug delivery are now predicated upon the rational design of polymers tailored
to specific cargo and engineered to exert distinct biological functions.
Polymers are both present and artificial . Among present polymers are proteins, starches, latex, and
cellulose. Synthetic polymers are produced on an outsized scale and have many properties and are
used.

Simple manipulation of the water solubility of polymers, by increasing their chain length through
cross‐linking or by hydrophobicity or hydrophilizing them with copolymers and other groups yield a
wealth of materials with a good spectrum of possible applications. The resulting materials are
capable of a spread of drug-enhancing functions.
Polymers can:

• Prolong drug availability if medicines are formulated as hydrogels or microparticles though.


• Favourably alter biodistribution, if formulated into dense nanoparticles.
• Enable hydrophobic drug administration if formulated as micelles though.
• Transport a drug to its usually inaccessible site of action if formulated as gene medicines though.
• Make drugs available in response to stimuli.

The pharmaceutical applications of polymers range from their use as binders though in tablets to
viscosity and flow controlling agents in liquids, suspensions, and emulsions though. Polymers are
often used as film coatings to disguise/mask the unpleasant taste of a drug, enhance drug stability,
and modify drug release characteristics. Pharmaceutical polymers are widely wont to achieve taste
masking; controlled release (e.g. extended, pulsatile, and targeted) enhanced stability though, and
improved bioavailability. Monolithic delivery devices are systems during which a drug is dispersed
within a polymer matrix and released by diffusion. the speed of the drug release from a matrix
product depends on the initial drug concentration and relaxation of the polymer chains which overall
displays a sustained-release characteristic.

The families of polymer constructs called polymer therapeutics

CLASSIFICATION POLYMERS
The basis on interaction with water

 Non‐biodegradable hydrophobic Polymers:‐ E.g. PVC,


 Soluble Polymers:‐ E.g. HPMC, PEG
 Hydro gels:‐ E.g. Polyvinyl pyrrolidine

Based on the polymerization method

 Addition Polymers:‐ E.g. Alkane Polymers


 Condensation polymers:‐ E.g. Polystyrene and Polyamide

Based on the polymerization mechanism

 Chain Polymerization
 Step growth Polymerization

Based on chemical structure

 Activated C‐C Polymer


 Inorganic polymers
 Natural polymers

Based on occurrence

 Natural polymers:‐ E.g. 1. Proteins‐collagen, keratin, albumin, cellulose


 Synthetic polymers:‐ E.g. Polyesters, polyamides

Based on bio‐stability

 Bio‐degradable
 Non-Bio-degradable
Characteristics of a perfect polymer

 It should be versatile and possess a good range of mechanical, physical, chemical properties.
 It should be non‐toxic and have good mechanical strength and will be easily administered.
 It should be inexpensive and straightforward to fabricate.
 It should be inert to host tissue and compatible with the environment.

Criteria followed in polymer selection

 The polymer should be soluble and straightforward to synthesize.


 It should have a finite relative molecular mass.
 It should be compatible with the biological environment.
 It should be biodegradable.
 It should provide good drug-polymer linkage.

ROLE OF POLYMER IN PHARMACEUTICAL DRUG DELIVERY

Immediate-release dosage forms

Tablets

Polymers are used for several years as excipients in conventional immediate‐release oral dosage
forms, either to assist within the manufacturing process or to guard the drug against degradation
upon storage. Microcrystalline cellulose is usually used as an alternative to carbohydrates as diluents
in tablet formulations of highly potent low‐dose drugs. Starch and cellulose are used as disintegrants
in tablet formulations, which swell on contact with water, leading to the tablet “bursting,” increasing
the exposed area of the drug and improving the dissolution characteristics of a formulation. Polymers
including polyvinyl‐pyrrolidone and hydroxypropyl methylcellulose (HPMC) also find uses as
binders that aid the formation of granules that improve the flow and compaction properties of tablet
formulations before tableting. Dosage forms must be coated with a “non-functional” polymeric film
coating to guard a drug against degradation though, mask the taste of an unpalatable drug or
excipients, or improve the visual elegance of the formulation without affecting the drug release rate
though.

Capsules

Capsules are used as an alternate to tablets, for poorly compressible materials, to mask the bitter taste
of certain drugs, or sometimes to extend bioavailability. Many of the polymeric excipients who want
to “bulk out” capsule fills are equivalent to those utilized in immediate‐release tablets. Gelatine has
been used almost exclusively as a shell material for hard (two‐piece) and soft (one‐piece) capsules
though. HPMC has recently been developed and accepted as an alternate material for the
manufacture of hard (two‐piece) capsules.

Release dosage forms

It is now generally accepted that for several therapeutic agents drug delivery using immediate release
dosage forms end in suboptimal therapy and/or systemic side effects. Pharmaceutical scientists have
attempted to beat the restrictions of conventional oral dosage forms by developing modified release
dosage forms.

Extended release dosage forms

The therapeutic effect of the medicine that has a brief biological half‐life could also be enhanced by
formulating them as extended or sustained release dosage forms. Extended and sustained release
dosage forms prolong the time that systemic drug levels are within the therapeutic range and thus
reduce the number of doses the patient must fancy maintaining a therapeutic effect thereby
increasing compliance. the foremost commonly used water‐insoluble polymers for extended‐release
applications are the ammonium methacrylate copolymers (Eudragit RS and RL), cellulose
derivatives ethylcellulose, cellulose ester, and polyvinyl derivative, PVA. Eudragit RS and RL differ
within the proportion of quaternary ammonium groups, rendering Eudragit RS less permeable to
water, whereas ethylcellulose is out there in several different grades of various viscosity, with
higher‐viscosity grades forming stronger and more durable films.

Gastroretentive Dosage Forms

Gastroretentive dosage forms offer an alternate strategy for achieving an extended-release profile,
during which the formulation will remain within the stomach for prolonged periods, releasing the
drug in place, which can then dissolve within the liquid contents and slowly pass into the tiny
intestine. Unlike a standard extended-release dosage form, which gradually releases the drug during
transit along the alimentary canal, such a delivery system would overcome the issues of medicine
that are absorbed preferentially from specific sites within the alimentary canal (for example, many
drugs are absorbed poorly from the distal gut, where an extended-release dosage form may spend the
bulk of its time), producing nonuniform plasma time profile delivery systems don't believe polymers
present, to realize gastro retention mucoadhesive and low‐density polymers are evaluated, with little
success thus far, for his or her ability to increase the gastric duration by bonding to the mucus lining
of the stomach and floating on top of the gastric contents respectively.

TYPES OF POLYMERS IN PHARMACEUTICAL DRUG DELIVERY

Polymers used as colon targeted drug delivery:

Polymers play a really important role within the colon-targeted drug delivery system. It protects the
drug from degradation or release within the stomach and little intestine. It also ensures an abrupt or
controlled release of the drug within the proximal colon.

Polymers within the mucoadhesive drug delivery system: The new generation mucoadhesive
polymers for buccal drug delivery with advantages like a rise within the duration of the polymer,
penetration enhancement, site-specific adhesion, and enzymatic inhibition, site-specific
mucoadhesive polymers will undoubtedly be utilized for the buccal delivery of a good sort of
therapeutic compounds. the category of polymers has enormous for the delivery of therapeutic
macromolecules.
Polymers for sustained release:

Polymers are utilized in the sustain by preparing biodegradable microspheres containing a


replacement potent osteogenic compound.

Polymers as floating drug delivery system:

Polymers are generally employed in floating drug delivery systems so on target the delivery of
medicine to a selected region within the alimentary canal i.e. stomach. Natural polymers which are
explored for his or her promising potential in stomach-specific drug delivery include chitosan,
pectin, xanthan gum, guar gum, gellan gum, ka kayagum, psyllium, starch, husk, starch, alginates,
etc.

Polymers in tissue engineering:

A wide range of natural origin polymers with a special specialize in proteins and polysaccharides
could be potentially useful as carriers systems for active biomolecules as cell carriers with the
application within the tissue engineering field targeting several biological tissues.

Literature Review
RECENT DEVELOPMENTS within the USE OF POLYMERS FOR DRUG DELIVERY
SYSTEMS

The oral drug delivery system has been in practice for several years because the most generally used
the root of administration among all the roots that are employed for the systemic delivery of
medicine via various pharmaceutical products for various dosage forms. an outsized of both
synthetic and natural are studied for possible application in drug delivery systems.

The most advantageous property of polymers is that they need to be most generally used nowadays.
Two promising synthetic polymers which are developed for biomedical applications form
polyvinylpyrrolidone and polyethylene glycol acrylate-based hydrogels though. Both of them are
biodegradable and forms copolymers with natural macromolecules though.

On the opposite side, natural polymers have the advantage of high biocompatibility and less
immunogenicity though. Special attention has been shown through gelatin and collagen which are
natural polymers. Other natural polymers include chitosan, alginate, starch pectin, casein, and
cellulose derivatives though. The composition of a number of the above natural polymers with
synthetic polymers give added advantages as carriers for drugs delivery by complimenting the
properties of every other though.

Hybrid copolymers of collagen with biodegradable synthetic polymers polyethylene glycol 6000 and
polyvinylpyrrolidone were developed for the controlled release of contraceptives some drugs have an
optimum range within which maximum benefit springs and concentrations above or below this range
are often toxic or produce no therapeutic belief it in the least though. On the opposite hand, the very
slow progress within the efficacy of the treatment of severe disease has suggested a growing need for
a multidisciplinary approach to the delivery of therapeutics to targets within the tissues. a
replacement idea on controlling the pharmacokinetics, pharmacodynamics, non-specific toxicity,
immunogenicity, bio recognition, and efficacy of medicine was generated though. These new
strategies often called drug delivery systems (DDS), are supported by interdisciplinary approaches
that combine pharmaceutics, polymer science, analytical chemistry, and biology.

Polymers are utilized in the traditional dosage forms like binders for enteric coated tablets which
mask the unpleasant taste, viscosity enhancers for controlling flow in liquids, gel preparation just in
case of semisolids, and also utilized in the preparation of transdermal patches.

APPLICATIONS OF POLYMERS IN DRUG DELIVERY:-

Application in conventional dosage forms:-

 Tablets:-As binders to mask unpleasant taste for enteric-coated tablets


 Liquids:- Viscosity enhancers For controlling the flow
 Semisolids:- In-gel preparation
 In Ointments
 In transdermal Patches

Engineered Polymers for Advanced Drug Delivery

Smart polymers: - Modern drug delivery technology has been made possible by advances in polymer
science. Advancement in polymer science and engineering has developed new polymers for well-
controlled delivery of therapeutic drugs though. one among them is going to be the smart polymer
(stimuli-sensitive polymer) though, which possesses active responsiveness to environmental signals
and changes the physicochemical property as designed. Physical properties (temperature,
ultrasound, light, electricity, mechanical stress) though, chemical (pH, ionic strength), and biological
signals (enzymes, biomolecules) are used as triggering stimuli.
Smart polymeric systems
Passive targeting supported the EPR effect uses a singular bodily property of a disease (physiological
targeting), while conjugation of targeting moiety to drug carriers may be a biochemical targeting
strategy. Smart polymeric systems also provide a targeting strategy though.

APPLICATION IN COSMETICS

Cosmetic compositions are disclosed for the treatment of hair or skin, characterized by a content of
the latest quaternary chitosan derivatives of the formula though. The chitosan derivatives have an
honest substantively, particularly to hair keratin, and convince have hair strengthening and hair
conditioning characteristics. e.g.; Hair setting lotion, Oxidation Hair-coloring Composition, Hair
toning Composition, Skin Cream, Hair-treatment Composition, Gel-form respectively.

APPLICATION IN MANUFACTURING

 Bottle
 Vials
 Syringes
 Baking material

GENERAL PHARMACEUTICAL APPLICATIONS

Increase stability of drug:

 Chitosan is used to extend the steadiness of the drug during which the drug is complexed
with chitosan and makes a slurry and kneading for 45 minutes until dough mass. This dough
mass is pass-through sieve no.16 and makes granules is totally stable at different conditions.
 Orthopedic patients:
 Chitosan may be a biopolymer that exhibits osteoconductive, enhanced wound healing, and
antimicrobial properties which make it attractive to be used as a bioactive Coating to enhance
Osseointegration of orthopedic and craniofacial implant devices. it's been proven to be useful
in promoting tissue growth in tissue repair and accelerating wound-healing and bone
regeneration.
 Enhanced bone formation by transforming protein
 Chitosan composite microgranules were fabricated as bone substitutes for the aim of
obtaining high bone-forming efficacy. The microgranules have the pliability to fill various
sorts of defect sites with closer packing. The interconnected pores formed spaces between the
microgranules though, which allowed new bone ingrowth and vascularization. additionally,
the reworking growth factor-beta 1 (TGF-pl) was incorporated into the micro granules so as
to enhance bone-healing efficacy. The chitosan microgranules were fabricated by dropping a
mixed solution into a NaOH/ethanol solution though. TGF-pl was loaded into the chitosan
microgranules by soaking the microgranules during a TGF-pl solution respectively.
Future Trend

Many researchers are working during this field and have developed many modified copolymers with
desirable functional groups, who visualize their use not just for controlled drug delivery systems but
also used for artificial organ lining, immunology testing, agents in drug targeting, chemical reactors,
and substrates for cell growth. the foremost potential opportunities for these polymers in controlled
drug delivery dwell the sector of responsive delivery systems, it's expected that within the future
even quite today, researchers and doctors will have a wealth of products using biodegradable
polymers which will help faster patient recovery and eliminate follow up surgeries. Looking to this
scenario and a good range of research, the entire use of those biodegradable polymers in drug
delivery applications is accessible shortly.

FUTURE DIRECTIONS IN POLYMER DRUG DELIVERY

The most exciting opportunities in polymer drug delivery dwell stage of responsive delivery systems,
with which it'll be possible to deliver drugs through implantable devices in response to a measured
blood level or to deliver a drug precisely to a targeted site though. Much of the event of novel
materials in controlled drug delivery is that specialize in the preparation and use of those responsive
polymers with specifically designed macroscopic and microscopic structural and chemical features.
Such systems include:

• Copolymers with desirable hydrophilic/hydrophobic interactions.


• Block or graft copolymers.
• Complexation networks responding via hydrogen or ionic bonding though.
• Dendrimers or star polymers as nanoparticles for immobilization of enzymes, drugs, peptides, or
other biological agents respectively.
• New biodegradable polymers.
• New blends of hydrocolloids and carbohydrate-based polymers though.

CONCLUSION
The use of novel polymers not only offers benefits but can also be harmful due to the toxicity and
other incompatibilities that accompany them though. Polymers possessing a singular strength within
their application towards drug delivery application which enables the new advancement in the
formulating new drug delivery systems which improves the therapy and treatment though.

Care should be taken to properly select polymers while designing a delivery system though. the last
word goal is to introduce cost-effective, biocompatible, multifunctional. less toxic polymers in order
that the delivery systems undergo the varied phases of clinical trials and benefit society. Among
various sorts of polymer hydrogels, polymer blends of natural and or synthetic polymer are utilized
in pharmaceutical formulations. therein controlled drug delivery systems having a plus over
conventional therapy fall under various categories like diffusion-controlled chemically controlled,
solvent activated, and modulated release systems. On the entire, polymers are being extensively
utilized in the pharmaceutical industry thanks to their vast applications.

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