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Carboxymethyl gum katira: synthesis, characterization and evaluation for nanoparticulate drug delivery

机译：Carboxymethyl Gum Katira：纳米颗粒药物递送的合成，表征和评价

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In the present study a carboxymethyl derivative of gum katira was synthesized and explored for drug delivery applications. Carboxymethyl functionalization was achieved by reacting it with monochloroacetic acid under alkaline conditions. The modified gum was found to have a degree of carboxymethyl substitution of 0.6. Carboxymethyl modification was confirmed by FT-IR study. Thermal studies revealed higher thermal stability, while X-ray diffraction patterns showed increase in crystallinity of the carboxymethyl derivative. SEM study showed that carboxymethylation changes thin flaky, smooth surface particles into polyhedral sharp edged particles with a rough surface. Further, the preparation of polyelectrolyte complex nanoparticles of carboxymethyl gum katira and chitosan was optimized using 2-factor, 3-level central composite experimental design. The optimal calculated parameters were concentrations of carboxymethyl gum katira (0.26%, w/v) and chitosan (0.03%, w/v), which provided polyelectrolyte nanoparticles of size 269 nm and ofloxacin entrapment of 83.65%. The nanosuspension was found to release 92% of ofloxacin in 24 h, following Higuchi's release kinetics with the mechanism of release being Super Case-II transport. An ophthalmic nanosuspension of ofloxacin (0.3%, w/v) formulated using the optimized batch showed slightly higher apparent corneal permeability of ofloxacin than the aqueous solution of ofloxacin across the isolated porcine cornea. Further, the histological studies on corneas treated with ophthalmic nanosuspension revealed corneal biocompatibility. In conclusion carboxymethyl gum katira possess an excellent potential for exploring polyelectrolyte nanoparticulate ocular drug delivery.
机译：在本研究中，合成胶Katira的羧甲基衍生物并探索药物递送应用。通过在碱性条件下使其与单氯酸乙酯反应来实现羧甲基官能化。发现改性的胶具有0.6的羧甲基取代度。通过FT-IR研究证实了羧甲基改性。热研究显示出较高的热稳定性，而X射线衍射图案显示羧甲基衍生物的结晶度的增加。 SEM研究表明，羧甲基化将薄的片状变化为具有粗糙表面的多面体锋利的颗粒。此外，使用2因子，3级中央复合实验设计优化了羧甲基胶Katira和壳聚糖的聚电解质复合纳米粒子的制备。最佳计算的参数是羧甲基胶Katira（0.26％，W / V）和壳聚糖（0.03％，W / V）的浓度，其提供大小269nm和氧氟沙星含量为83.65％的聚电解质纳米颗粒。发现纳米溶症释放在Higuchi的释放动力学中，在24小时内释放出92％的氧氟沙星，其释放动力学是超级案例-II运输的机制。使用优化分批配制的氟哌辛（0.3％，W / V）的眼科纳米悬浮液显示出氧氟沙星的表观角膜渗透性略高于整个猪角膜中氧氟沙星的水溶液。此外，用眼科纳米术治疗的角膜中的组织学研究揭示了角膜生物相容性。结论羧甲基胶Katira具有优异的探索聚电解质纳米颗粒眼药递送的潜力。

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  • 来源
    《RSC Advances》 |2015年第100期|共11页
  • 作者

    Minkal; Ahuja Munish; Bhatt D. C.;

  • 作者单位

    Guru Jambheshwar Univ Sci &

    Technol Dept Pharmaceut Sci Drug Delivery Res Lab Hisar 125001 Haryana India;

    Guru Jambheshwar Univ Sci &

    Technol Dept Pharmaceut Sci Drug Delivery Res Lab Hisar 125001 Haryana India;

    Guru Jambheshwar Univ Sci &

    Technol Dept Pharmaceut Sci Drug Delivery Res Lab Hisar 125001 Haryana India;

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