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Polymeric Based Drug Delivery System: Risa Ahdyani, M.Pharm - Sci

This document discusses polymeric drug delivery systems. It begins by defining polymers and their uses in pharmaceuticals. There are several classifications of polymers discussed, including soluble polymers, biodegradable polymers, and mucoadhesive polymers. Diffusion-controlled delivery systems and solvent-activated systems are also covered. The document outlines various polymer properties that can be modified, such as molecular weight and copolymer composition, to achieve desired drug release profiles. Smart polymers and examples of polymers used in drug delivery are also mentioned. In summary, the document provides an overview of polymer classification and characteristics as they relate to controlled drug delivery applications.

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Risa Ahdyani
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0% found this document useful (0 votes)
98 views26 pages

Polymeric Based Drug Delivery System: Risa Ahdyani, M.Pharm - Sci

This document discusses polymeric drug delivery systems. It begins by defining polymers and their uses in pharmaceuticals. There are several classifications of polymers discussed, including soluble polymers, biodegradable polymers, and mucoadhesive polymers. Diffusion-controlled delivery systems and solvent-activated systems are also covered. The document outlines various polymer properties that can be modified, such as molecular weight and copolymer composition, to achieve desired drug release profiles. Smart polymers and examples of polymers used in drug delivery are also mentioned. In summary, the document provides an overview of polymer classification and characteristics as they relate to controlled drug delivery applications.

Uploaded by

Risa Ahdyani
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Polymeric Based Drug Delivery System

Risa Ahdyani, M.Pharm.Sci


Apa itu polimer?
• the Food and Drugs Administration, rigorously control the standards of
these polymers to ensure that no adverse effects result from their use. As
a result of these considerations the cost of pharmaceutical polymers is
frequently more expensive than nonmedical polymers
• Polimersangat luas digunakan dalam bidang farmasetik untuk
pembuatan sediaan farmasi. Bagaimana pemilihan polimer?
Klasifikasi polimer
Pentingnya mengetahui sifat fisikokimia polimer
Karakteristik polimer yang diinginkan dapat dicapai dengan merubah sifat
fisikokimianya, seperti tipe polimer, BM polimer, struktur monomer, dan
kopolimerisasi.

1. Selulosa merupakan polimer yang tersedia dengan berbagai MW sehingga memberikan range
viskositas ketika diformulasikan dalam sediaan cair. Bagaimana pengaruhnya?
2. Certain polymethacrylates are soluble in alkaline pH making them suitable for enteric
coatings (coatings which do not dissolve in the stomach but dissolve in the more alkaline
regions of the gastrointestinal tract);
3. however by changing the copolymer composition the polymer may be rendered insoluble and
therefore used as an insoluble film coating for sustained release dosage forms.
Penggunaan polimer pada DDS konvensional
• Conventional drug delivery systems use doses of drugs in form of capsules,
tablets which are formed by compression, coating and encapsulation of
bioactive drug molecules.
• Polymers play a versatile role in such conventional formulations; they serve
as binding agents in capsules, film coating agents in tablets to mask the
unpleasant taste of the drug, to improve the stability of hydrophilic
drugs, and viscosity enhancers in emulsions and suspensions.
• Some of the polymers given along with bioactive drug molecules include
cellulose derivatives, poly (N-vinyl pyrrolidone) and poly (ethylene glycol)
PEG.
Polymer controlled delivery system
• The usefulness of polymers in drug delivery systems is well established.
Continued improvement and accelerating research and development in
polymeric materials has played a vital role in the progress of most
controlled- release technologies.
• In the past 25 years, there has been a considerable increase in interest in
this technology, as is shown by the increasing number of publications and
patents in the area of controlled drug-release systems using synthetic as
well as naturally occurring polymeric materials
• Due to rapid advances in recent years, the application of polymers to drug
delivery has grown considerably. In order to provide a better
understanding of the relationships and factors affecting various polymers,
we have divided research and development into the following areas:
1. Soluble polymers

2. Biodegradable or bioerodible polymers

3. Mucoadhesive polymers
Smart Polymers
1. Smart polymers are those which exhibit change depending upon the change
in environmental conditions. In medicine stimuli responsive polymers show
the change in their properties in response to the change in biological
conditions.
2. The various stimuli may be temperature, pressure, pH, electric field,
magnetic field, light, change in concentration, ionic strength, redox
potential etc.
3. Responses to such stimuli include dissolution, precipitation, swelling,
change in conformation, and change in hydrophobic and hydrophilic
properties.
4. There is change in pH along the GI tract which is considered during design of
oral drug delivery systems.
5. The cancerous tissue and swelled tissue show a drastic variation in pH.
Polymer bound drugs are released in such tissues due to deprotonation (acid
condition)/protonation (base condition) of complex polymer structure
under the conditions of altered pH
Contoh polimer
Klasifikasi berdasarkan mekanisme pelepasan
Currently available polymers for controlled release can be classified into
four major categories:
1. diffusion-controlled systems

2. solvent-activated systems

3. chemically controlled systems

4. magnetically controlled systems.


Diffusion-controlled systems
• In order to maintain uniformity of drug delivery, the thickness of the
polymer must be consistent. One of the problems with the reservoir
system is that such a system must be removed from the body after the
drug is depleted because the polymer remains intact. Another potential
problem is that if the reservoir membrane accidentally ruptures, a large
amount of drug may be suddenly released into the bloodstream (known
as “drug dumping”.
• In the matrix type of diffusion-control system, the drug is uniformly
distributed throughout the polymer matrix and is released from the
matrix at a uniform rate as drug particles dislodge from the polymer
network. In such a system, unlike the reservoir, there is no danger of drug
dumping in case of an accidental rupture of the membrane.
Solvent-activated systems
• Osmotically controlled systems
an external fluid containing a low concentration of a drug moves across a
semipermeable membrane to a region inside the device, where the drug is
in high concentration. Osmotic pressure tends to decrease the
concentration gradient between one side of the membrane and the other.
The inward movement of fluid forces the dissolved drug out of the device
through a small orifice
• swelling-controlled systems
In the swelling-controlled systems, the polymer holds a large quantity of
water without dissolving. The system consists of hydrophilic
macromolecules cross-linked to form a three-dimensional network. A
characteristic of such systems is their permeability, for low molecular
weight solutes, at a controlled rate as the polymer swells.
Chemically controlled systems
• The “pendant-chain” system
A “pendant chain system” is one in which the drug molecule is chemically linked
to the backbone of the polymer. In the body, in the presence of enzymes and
biological fluids, chemical hydrolysis, or enzymatic cleavage, occurs with
concomitant release of the drug at a controlled rate. The drug may be linked
directly to the polymer or via a “spacer group.”
• The bioerodible or biodegradable system.
The controlled release of the drug involves polymers that gradually decompose.
The drug is dispersed uniformly throughout the polymer and is slowly released
as the polymer disintegrates. Two major advantages of erodible systems are (1)
polymers do not have to be removed from the body after the drug supply is
exhausted, and (2) the drug does not have to be water-soluble. In fact, because of
these factors, future use of bioerodible polymers is likely to increase more than
any other type of polymer in the future.
Magnetically controlled systems
• Two major advantages of the magnetically responsive carrier system over
other drug delivery systems are its high efficiency for in vivo targeting
and its controllable release of a drug at the microvascular level.
• Selective targeting of antitumor agents, while minimizing toxic effects, has
been a major goal in cancer chemotherapy.
• Conventionally used systemic antineoplastic agents are unable to achieve
ideal tumor specificity.
• Magnetically responsive drug carrier systems, composed of albumin and
magnetic microspheres, have been developed for use in cancer
chemotherapy. Because of their magnetic characteristics, these
microspheres are theoretically capable of enhanced area-specific
localization
Polymeric drug/ polymer therapeutics
Polymer therapeutics is a term used to describe an increasingly
important area of biopaharmaceutics in which a linear or branched
polymer chain behaves either as the bioactive (a polymeric drug)
or, more commonly, as the inert carrier to which a therapeutic is
covalently linked, as in the case of polymer-drug conjugates,
polymer-protein conjugates, polymeric micelles, and
multicomponent polyplexes
Diffusion controlled system
Advantages
1. Polymers used in colloidal drug carrier systems, consisting of small particles, show great advantage in
drug delivery systems because of optimized drug loading and releasing property
2. A polymer (natural or synthetic) is aggregated with a drug in controlled drug delivery and hence it gives
a effective and controlled dose of dug avoiding overdose
3. The degradable polymers are ruptured into biologically suitable molecules that are assimilated and
discarded from the body through normal route.
4. Reservoir based polymers is advantageous in various ways like it increase the solubility of
incompetently soluble drugs and it lowers the antagonistic side effects of drugs
5. Magneto-optical polymer coated and targeted nanoparticles are multimodal (optical and MRI detection)
while Quantum Dots are only optically detectable.
6. Some Quantum dots contain Cd which is known to be toxic to humans. Magneto/optical nanoparticles
whether polymer coated or targeted are composed of iron oxides/polymers which are known to be safe,
therefore have great future.
TERIMAKASIH

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