Polymeric Drugs: A Novel Approach to Drug Delivery System




  • Pooja Chawla
  • Mishra


This review article describes the current status and recent advances of polymeric drugs with regard to their application in drug delivery system. Essentially polymer-drug conjugation aims to achieve improved drug targeting, decrease drug toxicity and overcome mechanisms of drug resistance. First generation conjugates used linear monomethoxy PEGs and other linear polymers. Modern polymeric chemistry is increasingly producing new polymeric architectures such as dendrimers, hyper branched polymers and hybrid macromolecular structures (such as star polymers, linear graft and dendronized linear polymers and novel therapeutic siRNA. This undoubtedly can be employed for designing of second generation polymer therapeutics. Clinical approval of products such as Copaxone®, Renagel®, Vivagel® and Welchol® have been successful in developing interest in polymer therapeutics as a growing field of research and development. In conclusion, there is emerging data that polymer drug conjugation has become useful in a wide range of treatments from infectious to chronic diseases such as cancer. Polymer therapeutics holds promising future applications in the field of nanotherapeutics. 

Polymeric Drugs: A Novel Approach to Drug Delivery System


Download data is not yet available.


Metrics Loading ...


Polymeric drugs, drug deliverY, dendrimers, PEGs, Clinical trials




How to Cite

Chawla P, Mis M. Polymeric Drugs: A Novel Approach to Drug Delivery System. Scopus Indexed [Internet]. 2013 May 31 [cited 2024 May 18];6(1):1925-34. Available from: https://www.ijpsnonline.com/index.php/ijpsn/article/view/603



Review Articles


Adams N and Schubert US (2007). Poly (2-oxazolines) in biological and biomedical application contexts. Adv Drug Deliv Rev 59: 1504-1520.

Albain KS, Belani CP, Bonomi P, O’ Byrne KJ, Schiller JH and Socinski M (2006). PIONEER: a phase III randomized trial of paclitaxel poliglumex versus paclitaxel in chemotherapy-naive women with advanced-stage non-small-cell lung cancer performance status of 2. Clin Lung Cancer 7: 417-19.

Akullian LC, Stevenson CA, Yurkovetskiy AV, Benson JD, Fram RJ and Lowinger TB (2009). Anti-angiogenic and anti- tumor activity of XMT-1107, A fumagillol – derived polymer conjugate, and its in vivo Release Product XMT-1191. Proc Am Assoc Cancer Res abstract 670.

Bonomi P (2007). Paclitaxel poliglumex (PPX, CT-2103): macromolecular medicine for advanced non-small cell lung cancer. Expert Rev Anticancer Ther 7: 415-422.

Beer NL, Gabe R, McCormack S, Kitchen VS, Lacey CJ and Nunn AJ (2002). Dextrin Sulfate as a vaginal microbicide: Randomized, Double-Blind, Placebo-Controlled Trial including Healthy Female Volunteers and Their Male Partners. JAIDS 30: 391-398.

Breslow DS (1976). Biologically active synthetic polymers, Pure & Appl Chem 46: 103–113.

Canal F, Sanchis J and Vicent MJ (2011). Polymer-drug conjugates as nano-sized medicines, Curr Opin Biotechnol 22: 894-900.

Davis FF (2002). The origin of pegnology. Adv Drug Deliv Rev 54: 457-458.

Davis ME (2009). Design and development of IT-101, a Cyclodextrin-containing Polymer Conjugate of Camptothecin, Adv Drug Deliv Rev 61: 1189.

Dipetrillo T, Milas L, Evans D, Akerman P, Nq T, Miner T, Cruff D, Chauhan B, Iannitti D, Harrington D and Safran H (2006). Paclitaxel poliglumex (PPX-Xyotax) and concurrent radiation for esophageal and gastric cancer: a phase I study. Am J Clin Oncol 29: 376-379.

Duncan R (2003). The drawing era of polymer therapeutics, Nat Rev Drug Discov 2: 347-360.

Duncan R (2003). Polymer–Drug Conjugates. In Handbook of Anticancer Drug Development (Budman DR, Calvert AH, Rowinsky EK, and Hill Bridget T, eds), pp. 239–260.

Duncan R, Gac-Breton S, Keane R, Musila R, Sat YN, Satchi R and Searle F (2001). Polymer-drug conjugates, PDEPT AND PELT: basic principles for design and transfer from the laboratory to clinic. J Control Release 74: 135-146.

Duncan R (2009). Development of HPMA copolymer anticancer conjugates: clinical experience and lessons learnt, Adv Drug Deliv Rev 61: 1131–1148.

Duncan R (2011). Polymer therapeutics as nanomedicines: new perspectives, Curr Opin Biotechnol 22: 492-501.

Duncan R, Gilbert H, Carbajo RJ, and Vicent MJ (2008). Polymer masked-unmasked protein therapy (PUMPT). 1. Bioresponsive dextrin-trypsin and -MSH conjugates designed for α -amylase activation. Biomacromolecules 9: 1146 -54.

Duncan R and Izzo L (2005). Dendrimer biocompatibility and toxicity. Adv Drug Deliv Rev 57: 2215 -37.

Fang J, Deng D, Nakamura H, Akuta T, Qin H, Iyer AK, Greish K and Maeda H (2008). Oxystress inducing antitumor therapeutics via tumor-targeted delivery of PEG-conjugated D-amino acid oxidase. Int J Cancer 122: 1135-1144.

Ferguson EL, Alshame AM and Thomas DW (2010). Evaluation of hyaluronic acid – protein conjugates for polymer masked – unmasked protein therapy, Int J Pharm 402: 95-102.

Gaspar R and Duncan R (2009). Polymeric carriers: preclinical safety and the regulatory implications for design and development of polymer therapeutics, Adv Drug Deliv Rev 61: 1220-1231.

Graham ML (2003). Pegasparaginase: a review of clinical studies. Adv Drug Deliv Rev 55: 1293-1302.

Greco F and Vicent MJ (2009). Combination therapy: Opportunities and challenges for polymer-drug conjugates as anticancer nanomedicines. Adv Drug Deliv Rev 61: 1203-1213.

Harris JM and Chess RB (2003). Effect of pegylation on pharmaceuticals. Nat Rev Drug Discov 2: 214–221.

Herth MM, Barz M, Jahn M, Zentel R and Rosch F (2010). 72/74As-labeling of HPMA based polymers for long-term in vivo PET imaging. Bioorg Med Chem Lett 20: 5454-5458.

Jaspers K, Versluis B, Leiner T, Dijkstra P, Oostendorp M, Van Golde JM, Post MJ and Backes WH (2011). MR Angiography of collateral arteries in a hind limb ischemia model: comparison between blood pool agent gadomer and small contrast agent Gd-DTPA. PLoS ONE 6: e16159.

Kapustyan T (2001). FDA approves new combination treatment for chronic hepatitis C virus infection. Caremark New Drug Review 2(31).

Kumar A and Wakelee H (2006). Second- and third-line treatments in non-small cell lung cancer. Curr Treat Options Oncol 7: 37-49.

Levy Y, Hershfield MS, Melia CF, Polmar SH, Scudiery D, Berger M and Sorensen RU (1988). Adenosine deaminase deficiency with late onset or recurrent infections: response to treatment with polyethylene glycol modified adenosine deaminase. J Pediatr 113: 312-317.

Li C, Yu DF, Newman RA, Cabral F, Stephens LC, Hunter N, Milas L and Wallace S (1998). Complete regression of well-established tumors using a novel water-soluble poly(L-glutamic acid)-paclitaxl conjugate. Cancer Res 58: 2404-2409.

Lammers T, Subr V, Ulbrich K, Peschke P, Huber PE, Hennink WE and Storm G (2009). Simultaneous delivery of doxorubicin and gemcitabine to tumours in vivo using prototypic polymeric drug carriers, Biomaterials 30: 3466-3475.

Markovsky E, Baabur-Cohen H, Eldar-Boock AE, Omer L, Tiram G, Ferber S, Ofek P, Polyak D, Scomparin A and Satchi-Fainaro R (2012). Administration, distribution, metabolism and elimination of polymer therapeutics. J Control Release 161: 446-460.

Meerum TJM (2001). Phase I clinical and pharmacokinetic study of PNU166945, a novel water soluble polymer-conjugated prodrug of paclitaxel. Anticancer Drugs 12: 315-323.

Menjoge AR, Rinderknecht A, Navath RS, Faridnia M, Kim CJ,Romero R, Miller RK and Kannan RM (2011). Transfer of PAMAM dendrimers across human placenta: prospects of its use as drug carrier during pregnancy. J Control Rel 150: 326-338.

Moreadith RW, Viegas TX, Standaert Dg, Bentley MD, Fang Z, Dizman B, Yoon K, Weimer R, Harris JM, Ravenscroft P, Johnston TH, Hill M and Brotchie JM (2012). SER-214, a novel polymer-conjugated rotigotine formulation affords greatly extended duration of anti-parkinsonian effect and enhanced plasma exposure following a single administration in rodents and primates, MDS, late breaking abstract 5.

Neggers SJCMM and Van der Lely AJ (2011). Combination treatment with somatostatin analogues and pegvisomant in acromegaly, Growth Horm IGF Res 21: 129-133.

Nucci ML, Shorr R and Abuchowski A (1991). The therapeutic values of poly (ethylene glycol)-modified proteins. Adv Drug Deliv Rev 6: 133-151.

O’ Brien M, Bonomi P and Langer C (2006). Analysis of prognostic factors in chemo-naïve patients with advanced NSCLC and poor performance status (PS): Cox regression analysis of two phase III trials [abstract]. JCO 24: 7113.

O’Byrne K, Bonomi P and Paz-Ares L (2005). Paclitaxel poliglumex vs. docetaxel for second-line treatment of non-small cell lung cancer (NSCLC): the STELLAR 2 phase III study [Abstract]. Eur J Cancer 3: PS13.

Papisov MI, Hiller A, Yurkovetskiy A, Yin M, Barzana M, Hillier S and Fischman AJ (2005). Semisynthetic hydrophilic polyals. Biomacromolecules 6: 2659- 70.

Pasut G, Guiotto A and Veronese FM (2004). Protein, peptide and non-peptide drug PEGylation for therapeutic application. Expert Opin Therap Patents 14: 859–894.

Regelson W and Parker G (1986). The routinization of intraperitoneal (intracavitary) chemotherapy and immunotherapy. Cancer Invest 4: 29-42.

Ringsdorf H (1975). Structure and properties of pharmacologically active polymers. J Poly Sci 51: 135-153.

Ross H, Bonomi P, Langer C, O’Brein M, Paz-Ares L, Sandler A, Socinski M, Oldham F and Singer J (2006). Effect of gender on outcome in two randomized phase III trials of paclitaxel poliglumex (PPX) in cheminaive patients with advanced NSCLC and poor performance status (PS2) [abstract]. JCO 24: 7039.

Sakai T, Lino S and Okuno T (2006). High response rates with peginterferon alfa-2a (40KD) (PEGASYS ® ) plus ribavirin (COPEGUS ® ) in treatment-naive Japanese chronic hepatitis C patients: a randomised, double-blind, multicentre, phase III trial. J Hepatol 44 (Suppl 2): S224-S225.

Satchi R, Connors TA and Duncan R (2001). PDEPT: polymer-directed enzyme prodrug therapy I. HPMA copolymer-cathepsin B and PK1 as a model combination. Br J Cancer 85: 1070-1076.

Satchi- Fainaro R, Hailu H, Davies JW, Summerford C and Duncan R (2003). PDEPT: Polymer- Directed Enzyme Prodrug Therpay. 2. HPMA Copolymer- β- lactamase and HPMA Copolymer – C- Dox as a Model Combination. Bioconjug Chem 14: 797-804.

Satchi-Fainaro R, Puder M, Davies JW, Tran HT, Sampson DA, Greene AK Corfas G and Folkman J (2004). Targeting angiogenesis with a conjugate of HPMA copolymer and TNP-470. Nat Med 10: 255-261.

Schoemaker NE, Van Kesteren C, Rosing H, Jansen S, Swart M, Lieverst J, Fraier D, Breda M, Pellizzoni C, Spinelli R, Grazia Porro M, Beijnen JH, Schellens JH and ten

Bokkel Huinink WW (2002). A Phase I and pharmacokinetic study of MAG-CPT, a water soluble polymer conjugate of camptothecin. Br J Cancer 87: 608-614.

Sharkey RM, Govindan SV, Cardillo TM and Goldenberg DM (2011a). Epratuzumab-SN-38: a new antibody-drug conjugate for the therapy of hematological malignancies. Mol Cancer Ther 11: 224-234.

Sharkey RM, Karacay H, Govidan V and Goldenberg DM (2011b). Combination radioimmunotherapy and chemoimmunotherapy involving different or the same targets improves therapy of human pancreatic carcinoma xenogratfs models. Mol. Cancer Ther 10: 1072-1081.

Shiah JG, Sun Y, Kopeckova CM, Peterson RC and Kopecek SJ (2001). Combination chemotherapy and photodynamic therapy of targetable N-2-hydroxypropyl) methacrylamide copolymer-doxorubicin/mesochlorin e6-OV-TL16 antibody immunoconjugates. J Control Rel 74: 249–253.

Unger C, Harzmann R, Muller C, Witt C, Roberts J and Sethuraman N (2005). Phase I dose escalating study of PEG-PGA and DON: A new amino acid depleting anti cancer drug approach [abstract]. JCO 23: 3130.

Vicent MJ and Duncan R (2006). Polymer conjugates: nanosized medicines for treating cancer. Trends Biotechnol 24: 39-47.

Vicent MJ (2007). Polymer – Drug Conjugates As Modulators of Cellular Apoptosis. The AAPS Journal 9: E200-E207.

Vicent MJ, Greco F, Nicholson RI, Paul A, Griffiths PC and Duncan R (2005). Polymer therapeutics designed for a combination therapy of hormone-dependent cancer. Angew Chem Int Ed 44: 4061-4066.

Viegas TX, Bentley MD, Harris JM, Fang Z, Yoon K, Dizman B, Weimer R, Mero A, Pasut G and Veronese FM 2011. Polyoxazoline: chemistry, properties, and applications in drug delivery. Bioconjug Chem 22(5): 976-986.

Walsh MD, Hanna SK, Sen J, Rawal S, Cabral CB, Yurkovetskiy AV, Fram RJ, Lowinger TB and Zamboni WC (2012). Pharmacokinetics and antitumor efficacy of XMT-1001, a novel, polymeric topoisomerase I inhibitor, in mice bearing HT-29 human colon carcinoma xenografts. Clin Cancer Res 18: 2591-2602.

Webster R, Didier E, Harris P, Siegel N, Stadler J, Tilbury L and Smith D (2007). PEGylated proteins: evaluation of their safety in the absence of definitive metabolism studies. Drug Metab Dispos 35 (1): 9–16.

Yurkovetskiy AV and Fram RJ (2009). XMT-1001, a novel polymeric camptothecin pro-drug in clinical development for patients with advanced cancer. Adv Drug Deliv Rev 61: 1193-202.

Zhao H, Rubio B, Sapra P, Wu D, Reddy P, Sai P, Martinez A, Gao Y, Lozanquiez Y, Longley C, Greenberger LM and Horak ID (2008). Novel prodrugs of SN38 using multi-arm polyethylene glycol (PEG) linkers. Bioconjug Chem 19: 849-859.


Cerulean Therapeutics: http://www.prnewswire.com/news-releases-test/cerulean-completes-enrollment-of-randomized-phase-2-study-of-crlx101-in-non-small-cell-lung-cancer-161062595.html, http://pharmabiz.com/NewsDetails.aspx?aid=69937&sid=2.

Fumagillin: http://www.drugs.com/clinical_trials/mersana-s-second-development-candidate-xmt-1107-shows-superior-pharmacokinetics-anti-tumor-activity-7028.html, http://clinicaltrials.gov/ct2/show/NCT01011972.

OPAXIO: http://www.celltherapeutics.com/pdf/opaxio_facts-4pg.pdf, http://www.celltherapeutics.com/pdf/ASCO2011OPAXIO.pdf.pdf.

Mersana Therapeutics: http://www.mersana.com/product-pipeline/ xmt-1001.php, http://clinicaltrials.gov/ct2/show/NCT00455052.

Serina Therapeutics: http://serinatherapeutics.com/ser203.shtml, http://serinatherapeutics.com/Serina%20Poster%20for%202012%20MDS%20conference%20-%20v3.pdf.