Polymers In Drug Delivery

Conventional forms of drug delivery generally rely on tablets, eye drops, ointments and intravenous solutions. Recently, a number of novel drug delivery technologies have developed. These newer technological development include drug modification by chemical means, career based drug delivery and drug entrapment in polymeric matrices or within pumps that are placed in desired bodily compartments. These technical development in drug delivery/targeting approaches improve the efficacy of drug therapy thereby improve human health. Still there are many infectious and other deadly diseases are uncured due to the problem encountered by formulation scientists in drug delivery approaches. There is a strong need to develop a proper delivery system to achieve the complete therapeutic effects of the existing drug molecules. Use of polymeric materials in novel drug delivery approaches has attracted the scientists. Polymer chemists and chemical engineers, pharmaceutical scientists are engaged in bringing out design predictable, controlled delivery of bio active agents. When the drug is delivered to the site of action by using polymer based drug delivery approaches the safety and bio compatibility is questionable. The characterization of biocompatible polymers is more focused in the field of formulation development and drug delivery approaches etc. the biodegradable polymers have properties of degrading in biological fluids with progressive release of dissolved or dispersed drug. There is various novel drug delivery approaches are developed in the pipeline of polymer based drug delivery approaches. The bio-safety and biocompatibility are the important characteristics needed for the use of polymers in the field of pharmaceutical formulation and in novel drug delivery approaches. The present paper review is focused in the advances of biodegradable polymers based drug delivery approaches.

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Comments

haritha8vvn's picture

hi Sandeep, ur ppt is gud and informatic, but I have a small doubt: In the alternating copolymer u hav mentioned that the chain is [A-B-A-B-A-B-] but my doubt is why is it arranged in that fashion only, alternating can also be [A-A-B-A-B-B-A-] than why such specific arrangement?

V V N Haritha

MPharm-Pharmaceutics

sandeep kumar16's picture

cross linking in polymers occurs when primary valence bonds are formed between separate polymer chain molecules .. Chains with only one type of monomer are known as homopolymers. If two or more different type monomers are involved, the resulting copolymer can have several configurations or arrangements of the monomers along the chain. The four main configurations are depicted
1.RANDOM COPOLYMERS : different monomers are randomly arranged within the polymer chains ..
2.ALTERNATING COPOLYMERS :different monomers show difinite ordered alternation .
3.BLOCKED COPLYMERS: different monomers are arranged in long blocks of each monomer ..
4.GRAFT COPLYMERS :appendages of one type of monomer are grafted to long chain of other.

[A-B-A-B-A-B] is an alternate copolymer and the arrangement [A-A-B-A-B-B-A-] is of random type.....

shreeshabhat's picture

hi sandeep, your presentation is good. But to point out one thing, your presentation deviates from the title which you have selected. There's very less information on how polymers can be used as a drug delivery carrier. Indeed polymers are a good option for drug delivery, but your presentation doesnot justify it!! so, keep in mind from now on,and hope this little piece of observation from my side will help you in the future. all the best!!

Shreesha V Bhat Ramanbhai Patel College of Pharmacy, Education campus Changa, Gujarat, India. http://www.pharmainfo.net/shreeshabhat
sandeep kumar16's picture

thank u very much fr u r suggestion .. i will concentrate more on my topic n will try to give full information in my future presentations ... thanks fr ur gr8 suggestion which will surely help me very much .

harrybasson's picture

Very interesting ppt
But dear is it safe to use polymerin varios types of dosage forms, have u checked about toxicity profile of polymers ,,and compatibilty

sandeep kumar16's picture

nice question.. well polymers can be used in various dosage forms n der would be not much affect of its toxicity n it is more compatible ..

harrybasson's picture

ok dear have u done any work on it

sandeep kumar16's picture

no specific work but had read much about the polymers and i would like to carry out work in the near future on it

shreeshabhat's picture

as you have mentioned that dendrimers are a source of drug delivery, what is the probability that it will deliver the drug to the specific site required?
another que:2) what kind of drugs can a dendrimer entrap?
3) has it been proved to be a safe mode of drug delivery??

Shreesha V Bhat Ramanbhai Patel College of Pharmacy, Education campus Changa, Gujarat, India. http://www.pharmainfo.net/shreeshabhat
sandeep kumar16's picture

In recent decades, dendrimers — free-shaped synthetic macromolecules — have garnered a great deal of scientific interest due to their unique molecular nanostructure. Used in a variety of scientific applications, the use of dendrimers is now widely regarded as a safer, more precise, and more effective way to practice medicine.

A preclinical example of this process has evolved though the creation
of targeted dendrimer therapy. Dendritic macromolecules, or dendrimers,
are uniformed spherical nano-structures ranging from 10 to 200
Angstroms in diameter. Dendrimers have been used as a backbone for the
attachment of several types of biological materials including folate. These
molecules can direct the dendrimers to locations where receptors are
expressed on tumor cell surfaces. Dendrimers can also be conjugated to
therapeutic molecules, such as methotrexate, allowing for efficacious
delivery and a higher dose load to tumor cells avoiding the systemic toxicity
of current therapeutic strategies.7
Dendrimers with folate and methotrexate have been shown to bind
to KB cells expressing high levels of folate binding protein. In animal
model studies targeted chemotherapy with dendrimers showed ten times
the efficacy and decreased toxicity compared to standard chemotherapy
with free drug.
Using this technology one can envision a multitude of devices
whereby both the targeted agent and the chemotherapeutic agent utilized
could be specifically modified to meet the need of the receptor characteristics
and physiological properties of an individual tumor. In support
of this concept, additional dendrimers which target epidermal
growth factor receptor (EGFR), prostate specific membrane antigen
(PSMA), and RGD peptides have been fabricated and tested as well as
conjugates with Taxol as the therapeutic arm. In this scenario, patient
tumors could be screened for their cell surface receptor levels in order
to make decisions regarding which therapeutic would have greatest
potential.

I hope ur satisfied with the answer .. thanks fr asking such an interesting question ...

kuldeepsoni's picture

its a really nice and artistic presentation..good job!!

sandeep kumar16's picture

thank s kuldeep sir ....

rashmipatil's picture

a very interesting ppt!

sandeep kumar16's picture

thank 's yaar fr ur appreciation

rashmipatil's picture

you are welcome!

vedikag's picture

nice presentation !
how is it carried out ?
wat abt its safety n outcome ?
Vedika Gulati
Team Infinity
"∞"

Vedika Gulati Team Infinity "∞" http://www.pharmainfo.net/blog/team-infinity

sandeep kumar16's picture

polymers are safe mode of drug delivery as they increase the bio availabilty of the drug n it has no or very less toxic effects ....

zarrinfaria's picture

It is agood presentation...
Can you please provide me some information regarding drug formulations that are in market based on polymer:drug delivery system?
Good day.....:))

sandeep kumar16's picture

polymers are used in various types of formulations such as tablets gels etc ..
some of d drugs that are marketed are Adegen for scid syndrome , zinostatin n stimalmer for hepatocellular carcinoma, oncaspar for acute lymphoblastic leukamia, PEG INTRON for cancer ,multiple sclerosis,HIV/AIDS , PEGASYS
for hepatitis c.. etc.
thanks for ur quiery hope u satisfied ..

You have explained well about the thing

sandeep kumar16's picture

thanks fr ur appreciation n i m very happy dat u considered mine as d best one .. thanks yaar

nice ppt....but lacking information on polymer used in DDS...what is the cost effectiveness of polymer based DDS? Can population in India afford it?Give some example of polymer based DDS present in market?

majumdarshiv's picture

My Page : http://www.pharmainfo.net/majumdarshiv

I like your presentation.

Which are the newer methods available for studying Drug-polymer interaction other than DSC?

juhis's picture

what abt the stability and assurity in a polymer drug deleivery system?
Juhi Sharma
Team Infinity
"∞"

sandeep kumar16's picture

The drug will be released over time either by diffusion out of the polymer matrix or by degradation of the polymer backbone.

The continuous release of drugs from the polymer matrix could occur either by diffusion of the drug from the polymer matrix, or by the erosion of the polymer (due to degradation) or by a combination of the two mechanisms. For a given drug, the release kinetics from the polymer matrix are governed predominantly by three factors, viz. the polymer type, polymer morphology and the excipients present in the system.

The three main advantages of polymers are

1. Localized delivery of drug: The product can be implanted directly at the site where drug action is needed and hence systemic exposure of the drug can be reduced. This becomes especially important for toxic drugs which are related to various sytemic side effects (such as the chemotherapeutic drugs).
2. Sustained delivery of drugs: The drug encapsulated is released over extended periods and hence eliminates the need for multiple injections. This feature can improve patient compliance especially for drugs for chronic indications, requiring frequent injections (such as for deficiency of certain proteins).
3. Stabilization of the drug: The polymer can protect the drug from the physiological environment and hence improve its stability in vivo. This particular feature makes this technology attractive for the delivery of labile drugs such as proteins.

these ensure the drug delivery to my knowledge

komal nikam's picture

Nice work!!!!

I would like to ask you some questions these are-

1.What are recent development in this tech?
2.What are advantage ?
3.limitations of it ?

4.How polymers act as carrier eg:Cyclodextrine?

BEST LUCK!!!
KOMAL

sandeep kumar16's picture

i have answered abt d advantages to madhuri n discussing abt d disadvantages let me poing out dis ,,,,,, polymer carrier systems ,Compared to liposomes, which are basically empty vesicles that can be "stuffed full of drug," polymers have a low drug-carrying capacity. The payload that each polymer molecule can carry depends on the number of reactive groups where the drug can be attached. PEG, for example, can carry only two drug molecules, but other polymers can carry as much as 25 wt %,

Recent advances : New approaches to malignant glioma are being actively investigated. Local drug delivery directly to the site of the tumor is one novel approach that has been approved by the US FDA and other regulatory agencies worldwide. This agent, Gliadel delivers the chemotherapeutic drug carmustine (BCNU) from a biodegradable polymer placed in the resection cavity after brain tumor surgery. Gliadel represents the first clinical application of polymer delivery for brain tumors, but the potential for this new methodology is far greater.Clinical trials exploring the maximum-tolerated dose and the combination of Gliadel with systemic chemotherapeutic treatments such as temozolamide and O 6–benzylguanine are being reviewed. Finally, preclinical work on the efficacy of polymeric methods for delivering other chemotherapeutic agents, and a variety of novel compounds that modify brain tumor biology are being carried out . This latter work represents potential future clinical applications of local polymeric drug delivery to the brain and other sites where cancers can occur. to my knwoledge dis is d recent advancement in d field of polymers in drug delivery ..

komal nikam's picture

Which are compatibility criteria For selection of polymers in formulation & how it play imp. role?

BEST LUCK!!!
KOMAL

sandeep kumar16's picture

polymer-drug compatibility are carried out by physicochemical analyses of polymer-drug pairs and compared the difference in total and partial solubility parameters of polymer and drug. The partial and total solubility parameters for the polymer and drug were calculated using the group contribution method. Drug-polymer pairs with different enthalpy of mixing values were analyzed by physicochemical techniques including X-ray diffraction and Fourier transform infrared. Polymers identified to be compatible [i.e., polycaprolactone (PCL) and poly-β-benzyl-L-aspartate (PBLA)] and incompatible [i.e., poly (d,l-lactide (PLA)], by the above mentioned methods, were used to formulate Ellipticine. Specifically, Ellipticine was loaded into PBLA, PCL, and PLA films using a solvent casting method to produce a local drug formulation; while, polyethylene oxide (PEO)-b-polycaprolactone (PCL) and PEO-b-poly (d,l-lactide) (PLA) copolymer micelles were prepared by both dialysis and dry down methods resulting in a formulation for systemic administration.

Kaushalpathak's picture

very good slides and the topic as well. No doubt that these polymers are coming up very quickly may be because of its cost effectiveness and efficient drug delivery but can throw some light on its toxicity profile for long term use? In general, what are its common disadvantages?
Thanx :-)

sandeep kumar16's picture

The potential disadvantages include the possible toxicity or nonbiocompatibility of the materials used, undesirable by-products of degradation, any surgery required to implant or remove the system, the chance of patient discomfort from the delivery device, and the higher cost of controlled-release systems compared with traditional pharmaceutical formulations.

Abhamajumdar's picture

Hello Sandeep,
the topic of the presentation is "POLYMERS IN DRUG DELIVERY" but my dear boy there is hardly any information about the applications of polymers in drug delivery..you talk about pipes, lubcricants ,catalysts,flocculating agents,motor oil (is it mechanics?) ,fabric,viscosity modifier ,soda bottles,milk jugs,automobile contruction,helicopter blades.....i mean where are you lost?...your presentation revolves around polymers not their phamaceutical applications..why??...Please review the whole topic again..your abstract is good but your presentation contains NOTHING related to the abstract. ...i agree with himanshu saraubh ..

Mrs Abha Majumdar
Associate Professor

sandeep kumar16's picture

Thanks fr ur valuable comment . I concentrated more on d basic for discussing wat actually the poymer is and its uses and i have provided information on the drug delivery too while discussing about the dendrimers..
Mam if u want to know more abt the drug delivery drop ur queries so that i will try my level best to discuss about ur quieries .
Thanks mam

carizma_sha's picture

A reasonably good effort ! Although there is quite less information about the drug delivery, i would like to know:
a) How does the polymer branching have a sbstantive effect on its properties?

b) what ,acording to you are the characteristics of an "IDEAL" drug delivery system?

c) what are "BIODEGRADABLE POLYMERS" and how are the harmful byproducts eliminated from the body when these are used for drug delivery?

d) In your opinion, what is the "ONE GREATEST" (i am asking for onlyone) advantage of polymer drug delivery system...give reasons in support of yor answer

e)what are the various factors afecting the biodegradation of polymers once they are inside the body?

sandeep kumar16's picture

a)polymers science is developing enourmously n the use of polymers in drug delivery is vast .. This polymer branchin will affect the physicochemical properties and the availability of drugs in aqueous drug formulations containing water-soluble polymers in which polymers are binded to d drugs .

b)localised delivery of drug, sustained delivery of drug and stabilisation of drugs are the charactersitics of "ideal " drug delivery system ...

c)Homopolymers, co-polymers, block co-polymers, waxes and gelsare: biodegradable, compatible with a variety of drugs; are solid at temperatures; between 20° and 37° C.; are liquid at 38°-52° C.; and have the capacity to melt and resolidify without additional chemical reactions at these temperatures and can be formed in laboratory and used without the need for further chemical interaction.
Most biodegradable polymers are designed to degrade as a result of hydrolysis of the polymer chains into biologically acceptable, and progressively smaller, compounds. In some cases—as, for example, polylactides, polyglycolides, and their copolymers—the polymers will eventually break down to lactic acid and glycolic acid, enter the Kreb's cycle, and be further broken down into carbon dioxide and water and excreted through normal processes

d)In my opinion localised delivery of drug is the one greatest advantage of polymer drug delivery system , because the product can be implanted directly at the site where drug action is needed and hence systemic exposure of the drug can be reduced. This becomes especially important for toxic drugs which are related to various sytemic side effects (such as the chemotherapeutic drugs).
e)The continuous release of drugs from the polymer matrix could occur either by diffusion of the drug from the polymer matrix, or by the erosion of the polymer (due to degradation) or by a combination of the two mechanisms. For a given drug, the release kinetics from the polymer matrix are governed predominantly by three factors, viz. the polymer type, polymer morphology and the excipients present in the system. These are the three afactors on which the polymer degradtion depends..

thanks for askin question hope u satisfied with the answer

madhuri's picture

your ppt is intresting but some wat confusing. ok can tell me that how far it is applicable in drug delivery system and u have not given complete information or idea of ur topic.

madhuri
sandeep kumar16's picture

Polymer carriers have several advantages over other delivery methods such as liposomes and antibodies...Liposomes--spherical vesicles made of phospholipids--are particles, they get taken up by macrophages. High levels can be found in the liver and spleen, even when the liposomes are given "stealth" characteristics by coating them with PEG. In addition, stealth liposomes have other side effects, such as extravasation, in which the liposome moves from the blood vessel into tissue where it's not wanted. Antibodies, meanwhile, have the disadvantage that most receptors on tumor cells are also present on normal cells, making it hard to find ones that are unique to cancer.

In contrast, water-soluble polymers allow to work with a single molecule rather than a large particle. "You can choose a material which doesn't go to the liver and the spleen and to which you can bind an anticancer agent using a linkage that's designed to be more specifically clipped at the tumor tissue," . "It's in effect a macromolecular prodrug."

When Uncharged hydrophilic polymers, such as PEG and N-(2-hydroxypropyl) methacrylamide are hydrated, they can circulate in the blood for periods of up to about 24 hours..

ANOTHER ADVANTAGE of polymers is that the linkage can be designed to control where and when the drug is released. use of peptide linkages, which are cleaved after the polymer-drug conjugate is taken up into cells by the process of endocytosis. Within the resulting endosome, a family of enzymes called the lysosomal thiol-dependent proteases catalyzes the cleavage of the polymer-drug connection.

Sirisha Pingali's picture

hello mr.sandeep,,,,
Your work on Polymers in drug delivery system is very informative....but does these polymers can induce their action under normal body conditions??

Team: THE COGNITIVE MOLECULES....

Sirisha Pingali

http://www.pharmainfo.net/sirisha

Viswanadha Institute of Pharmaceutical Sciences.

www.vnips.edu.in

sandeep kumar16's picture

polymers are being widely used for their targetted release of drugs n more over these can induce their action under normal body conditions to my knowledge .Polymers are now widely used in various formulations for drug delivery .

gangadhar hari's picture

Hey thats really a novel topic.

Are there any formulations or marketed drugs using this DDS?

Regards,

""PHARMA TROJANS""
http://www.pharmainfo.net/gangadhar-hari

sandeep kumar16's picture

some of d drugs that are marketed are Adegen for scid syndrome , zinostatin n stimalmer for hepatocellular carcinoma, oncaspar for acute lymphoblastic leukamia, PEG INTRON for cancer ,multiple sclerosis,HIV/AIDS , PEGASYS
for hepatitis c.. etc.
thanks for ur quiery hope u satisfied ..

gangadhar hari's picture

That's great way of explanation Thank u very much &
All the best

Regards,

""PHARMA TROJANS""
http://www.pharmainfo.net/gangadhar-hari

Jasmine Jose's picture

Hiee Sandeep!
good work...ur ppt contains a lot of information on polymers!
Can u giv a brief outlook on its drug delivery aspects as the title says?
What are the various formulations available in the market?
How affordable is it to the common man?
Team-The Cognitive Molecules

sandeep kumar16's picture

The drug will be released over time either by diffusion out of the polymer matrix or by degradation of the polymer backbone.

The continuous release of drugs from the polymer matrix could occur either by diffusion of the drug from the polymer matrix, or by the erosion of the polymer (due to degradation) or by a combination of the two mechanisms. For a given drug, the release kinetics from the polymer matrix are governed predominantly by three factors, viz. the polymer type, polymer morphology and the excipients present in the system.

polymers are used in different type of formulations such as tablets ,gels ,etc...
polymers is developing science n it has many pharmaceuitcal applications .. Future developments in pharmaceutical applicantions will make it accessible to use even by the common man....

kishore.reddy's picture

Good work.
I have one question. Whether this type of drug delivery provide any long term side effects.

sandeep kumar16's picture

polymers science is emerging in d recent times n are used in various formulations for targetted drug delivery .. They have no side affects n very less toxic affects ..
to my knowledge

ur topic is very very intresting and worth knowing.

I would be happy to know whether there are any formulation available based on this concept
best luck
Panacea group

K.H.Patel.
My profile link is
http://www.pharmainfo.net/khushbu-hasmukh-patel

sandeep kumar16's picture

EUDRAGIT, EUPERGIT, PLASTOID, EUDRAPULSE, EUDRACOL and EUDRAMODE are some of the formulations available in the market .
thanks yaar

You have taken approach from the basics,good and how about characteristics of the stereoisomers of the available natural and synthetic polymers?

Regards,

"PHARMERS"
http://www.pharmainfo.net/santosh-kumar-jh

great job........
does this has any side effects ..? can u provide more information ?

saahithi

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