Entity

Time filter

Source Type


Paramjot,Nanomedicine Research Laboratory | Khan N.M.,Nanomedicine Research Laboratory | Kapahi H.,Nanomedicine Research Laboratory | Kumar S.,Polymer Chemistry and Technology Research Laboratory | And 3 more authors.
Journal of Drug Targeting | Year: 2015

Polymers have been utilized to deliver the drug to targeted site in controlled manner, achieving the high-therapeutic efficacy. Polymeric drug conjugates having variable ligands as attachments have been proved to be biodegradable, stimuli sensitive and targeted systems. Numerous polymeric drug conjugates having linkers degraded by acidity or intracellular enzymes or sensitive to over expressed groups of diseased organ/tissue have been synthesized during last decade to develop targeted delivery systems. Most of these organs have number of receptors attached with different cells such as Kupffer cells of liver have mannose-binding receptors while hepatocytes have asialoglycoprotein receptors on their surface which mainly bind with the galactose derivatives. Such ligands can be used for achieving high targeting and intracellular delivery of the drug. This review presents detailed aspects of receptors found in different cells of specific organ and ligands with binding efficiency to these specific receptors. This review highlights the need of further studies on organ-specific polymer-drug conjugates by providing detailed account of polymeric conjugates synthesized till date having organ-specific targeting. © 2015 Informa UK Ltd. Source


Sharma R.,Polymer Chemistry and Technology Research Laboratory | Sharma R.,Uttarakhand Technical University | Rawal R.K.,Polymer Chemistry and Technology Research Laboratory | Rawal R.K.,University of Georgia | And 2 more authors.
Bioorganic and Medicinal Chemistry | Year: 2014

Colon-specific azo based polyphosphazene-anticancer drug conjugates (11-18) have been synthesized and evaluated by ex-vivo release studies The prepared polyphosphazene drug conjugates (11-18) are stable in acidic (pH = 1.2) buffer which showed that these polymer drug conjugates are protected from acidic environment which is the primary requirement of colon specific targeted drug delivery The ex-vivo release profiles of polyphosphazene drug conjugates (11-18) have been performed in the presence as well as in the absence of rat cecal content The results showed that more than 89% of parent drugs (methotrexate and gemcitabine) are released from polymeric backbone of polyphosphazene drug conjugates (14 and 18) having n-butanol (lipophilic moiety) The in-vitro cytotoxicity assay has also been performed which clearly indicated that these polymeric drug conjugates are active against human colorectal cancer cell lines (HT-29 and COLO 320 DM) The drug release kinetic study demonstrated that Higuchi's equation is found to be best fitted equation which showed that release of drug from polymeric backbone as square root of time dependent process based on non-fickian diffusion Therefore, the synthesized polyphosphazene azo based drug conjugates of methotrexate and gemcitabine are the potential candidates for colon targeted drug delivery system with minimal undesirable side effects © 2014 Elsevier Ltd All rights reserved. Source


Kumar S.,Polymer Chemistry and Technology Research Laboratory | Kumar S.,Punjab Technical University | Murthy R.S.R.,Polymer Chemistry and Technology Research Laboratory | Bhardwaj T.R.,Polymer Chemistry and Technology Research Laboratory | Bhardwaj T.R.,Panjab University
Pharmaceutical Research | Year: 2015

Purpose: The synthesis and evaluation of novel biodegradable poly(organophosphazenes) (3–6) namely poly[bis-(2-propoxy)]phosphazene (3) poly[bis(4-acetamidophenoxy)]phosphazene (4)poly[bis(4-formylphenoxy)]phosphazene (5) poly[bis(4-ethoxycarbonylanilino)]phosphazene (6) bearing various hydrophilic and hydrophobic side groups for their application as nonocarrier system for antimalarial drug delivery is described.Methods: The characterization of polymers was carried out by IR, 1H-NMR and 31P-NMR. The molecular weights of these novel polyphosphazenes were determined using size exclusion chromatography with a Waters 515 HPLC Pump and a Waters 2414 refractive index detector. The degradation behavior was studied by 200 mg pellets of polymers in phosphate buffers pH 5.5, 6.8 and 7.4 at 37°C. The degradation process was monitored by changes of mass as function of time and surface morphology of polymer pellets. The developed combined drugs nanoparticles formulations were evaluated for antimalarial potential in P. berghei infected mice.Results: These polymers exhibited hydrolytic degradability, which can afford applications to a variety of drug delivery systems. On the basis of these results, the synthesized polymers were employed as nanocarriers for targeted drug delivery of primaquine and dihydroartemisinin. The promising in vitro release of both the drugs from nanoparticles formulations provided an alternative therapeutic combination therapy regimen for the treatment of drug resistant malaria. The nanoparticles formulations tested in resistant strain of P. berghei infected mice showed 100% antimalarial activity.Conclusions: The developed nanocarrier system provides an alternative combination regimen for the treatment of resistant malaria. © 2015 Springer Science+Business Media New York Source


Singla N.,Polymer Chemistry and Technology Research Laboratory | Sharma R.,Polymer Chemistry and Technology Research Laboratory | Bhardwaj T.R.,Polymer Chemistry and Technology Research Laboratory
Letters in Drug Design and Discovery | Year: 2014

The different substituted polyphosphazene-linked azo prodrug of Methotrexate (9-12) and chitosan-linked azo prodrug of methotrexate (13) were synthesized and characterized by modern analytical techniques such as IR, 1H NMR, 31P NMR and GPC. The in-vitro stability study showed that all polymeric drug conjugates are stable in upper GIT (pH = 1.2) and small intestine (pH = 7.4). In-vitro drug release showed that polyphosphazene-linked azo prodrug of methotrexate (12) has maximum release (88.4%) in the presence of rat cecal content compared to chitosan linked azo prodrug of methotrexate (13). Therefore, the synthesized polyphosphazene linked azo based drug conjugates of methotrexate (9-12) are the potential candidates for colon targeted drug delivery system with minimal undesirable side effects. © 2014 Bentham Science Publishers. Source


Kumar S.,Polymer Chemistry and Technology Research Laboratory | Singh R.K.,Polymer Chemistry and Technology Research Laboratory | Murthy R.S.,Polymer Chemistry and Technology Research Laboratory | Bhardwaj T.R.,Polymer Chemistry and Technology Research Laboratory
Pharmaceutical research | Year: 2015

PURPOSE: The synthesis and evaluation of novel biodegradable poly(organophosphazenes) (3-6) namely poly[bis-(2-propoxy)]phosphazene (3) poly[bis(4-acetamidophenoxy)]phosphazene (4)poly[bis(4-formylphenoxy)]phosphazene (5) poly[bis(4-ethoxycarbonylanilino)]phosphazene (6) bearing various hydrophilic and hydrophobic side groups for their application as nonocarrier system for antimalarial drug delivery is described.METHODS: The characterization of polymers was carried out by IR, (1)H-NMR and (31)P-NMR. The molecular weights of these novel polyphosphazenes were determined using size exclusion chromatography with a Waters 515 HPLC Pump and a Waters 2414 refractive index detector. The degradation behavior was studied by 200 mg pellets of polymers in phosphate buffers pH 5.5, 6.8 and 7.4 at 37°C. The degradation process was monitored by changes of mass as function of time and surface morphology of polymer pellets. The developed combined drugs nanoparticles formulations were evaluated for antimalarial potential in P. berghei infected mice.RESULTS: These polymers exhibited hydrolytic degradability, which can afford applications to a variety of drug delivery systems. On the basis of these results, the synthesized polymers were employed as nanocarriers for targeted drug delivery of primaquine and dihydroartemisinin. The promising in vitro release of both the drugs from nanoparticles formulations provided an alternative therapeutic combination therapy regimen for the treatment of drug resistant malaria. The nanoparticles formulations tested in resistant strain of P. berghei infected mice showed 100% antimalarial activity.CONCLUSIONS: The developed nanocarrier system provides an alternative combination regimen for the treatment of resistant malaria. Source

Discover hidden collaborations