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Although paclitaxel is a front-line chemotherapeutic agent for the treatment of metastatic breast cancer, its intravenous therapy produces deleterious adverse effects. In an attempt to address the issue, the present study aimed to develop a paclitaxel loaded thermosensitive/thermoresponsive hydrogel (PTXNp-TGel) for loco-regional administration to breast tumors to provide dose-dense chemotherapy. Poloxamer and xanthan gum were used to prepare TGel by the cold method. In vitro and in vivo performance of PTXNp-TGel was compared with TGel, pure drug loaded TGel (PTX-TGel) and marketed formulation, Taxol®. The formulated PTXNp-TGel showed acceptable gelation temperature and time (37 °C and 57 s), lower viscosity at room temperature and higher viscosity at body temperature to support sol-gel transition with increasing temperature, and sustained drug release up to 21 days. Additionally, PTXNp-TGel showed negligible hemolytic toxicity as compared to PTX-TGel and Taxol®. Intratumoral administration of PTXNp-TGel produced significantly higher antitumor activity as indicated by lowest relative tumor volume (1.50) and relative antitumor proliferation rate (27.71 %) in comparison with PTX-TGel, Taxol®, and PTXNp (p < 0.05). Finally, insignificant body weight loss during the experimental period, lack of hematotoxicity, nephrotoxicity, and hepatotoxicity imply improved therapeutic performance of the locally administrated dose-dense therapy of PTXNp-TGel as compared to Taxol®. • Paclitaxel loaded thermoresponsive hydrogel (PTXNp-TGel) provided dose dense chemotherapy in breast cancer model. • Xanthan gum provided mucoadhesive character to PTXNp-TGel and helped in retention of gel at the tumor site. • Loco regional administration of PTXNp-TGel exhibited remarkable antitumor activity without any significant side effects. • Same delivery system can be used for other cytotoxic agents to improve their therapeutic efficacy. [ABSTRACT FROM AUTHOR]

The effect of Ca 2+ ion cross-linker on acryalamide grafted carboxymethyl xanthan gum (CMXG-g-PAAm) on the drug release was investigated. Previously, CMXG was synthesized from XG and further grafted to CMXG-g-PAAm to retard the drug release. Once the CaCl 2 solution is added to CMXG-g-PAAm, Ca 2+ considerably affected the drug release mechanism mainly by diffusion and erosion. In order to validate the grafted polymer, tablets were prepared using wet granulation and dry granulation methods It has been noticed that the tablets prepared by wet granulation successfully controls the release of the drug over an extended period of time. Moreover, the release profile was aligned to Korsmeyer–Peppas equation and exhibited the drug transport mechanism via diffusion and erosion. [ABSTRACT FROM AUTHOR]

In the present work, an unreported graft copolymer of carboxymethyl xanthan gum and acrylamide has been synthesised by free radical polymerisation in a nitrogen atmosphere using ammonium persulphate as an initiator. The optimum reaction conditions adopted for affording maximum percentage of grafting including its grafting efficiency were obtained by varying the concentration of carboxymethyl xanthan gum from 4 to 24 g dm −3 ; ammonium persulphate from 5 × 10 −4 to 30 × 10 −4 mol dm −3 ; acrylamide from 0.4 to 1.2 mol dm −3 ; reaction temperature from 55 to 75 °C and reaction time from 30 to 90 min. The synthesised graft copolymer has been characterised by 1 H NMR, FTIR spectroscopy, X-ray diffraction measurement, thermal analysis, viscosity measurement and scanning electron microscopy. However, grafting of acrylamide onto carboxymethyl xanthan gum backbone enhanced its thermal stability. This graft copolymer might be well exploited globally as a potential carrier for drug delivery system. [ABSTRACT FROM AUTHOR]