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Design and formulation of polymeric nanosponge tablets with enhanced solubility for combination therapy

机译：聚合物纳米末期片剂的设计与配制，具有增强的组合治疗溶解度

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摘要

Three drugs namely caffeine, paracetamol, and aceclofenac are commonly used for treating various acute and chronic pain related ailments. These 3 drugs have varied solubility profiles, and formulating them into a single tablet did not have the desired dissolution profile for drug absorption. The objective of the present research was to tailor the drug release profile by altering drug solubility. This was achieved by loading the drug into nanosponges. Here, three-dimensional colloidal nanosponges were prepared using beta-cyclodextrin with dimethyl carbonate as a cross-linker using the hot-melt compression method. The prepared nanosponges were characterized by FTIR, H-1 NMR spectroscopy, DSC, XRPD studies and SEM. The FTIR and DSC results obtained indicated polymer-drug compatibility. The H-1 NMR spectroscopy results obtained indicated the drug entrapment within nanosponges with the formation of the inclusion complex. XRPD studies showed that the loaded drug had changed crystalline properties altering drug solubility. SEM photographs revealed the porous and spongy texture on the surface of the nanosponge. Box-Behnken experimental design was adopted for the optimization of nanosponge synthesis. Among the synthesized nanosponges containing paracetamol, aceclofenac and caffeine, batch F3-P31, F3-A31 and F3-C31 were considered optimized. Their particle size was 185, 181 and 199 nm with an entrapment efficiency of 81.53, 84.96, and 89.28% respectively. These optimized nanosponges were directly compressed into tablets and were studied for both pre and post-compression properties includingin vitrodrug release. The prepared tablet showed desired drug dissolution properties compared to the pure drug. The above outcomes indicated the applicability of nanosponges in modulating the drug release with varied solubility for combination therapy.
机译：三种药物即咖啡因，乙酰氨基酚和醋氯芬酸通常用于治疗各种急性和慢性疼痛的相关疾病。这3种药物具有不同的溶解性曲线，并将它们配制成单个片剂没有所需的溶解曲线以用于吸毒。本研究的目的是通过改变药物溶解度来定制药物释放型材。这是通过将药物加载到纳米龙中来实现的。这里，使用β-环糊精使用β-环糊精与碳酸二甲酯作为交联剂制备三维胶体纳米龙，使用热熔熔体压缩方法。通过FTIR，H-1 NMR光谱，DSC，XRPD研究和SEM表征制备的纳米孔。获得的FTIR和DSC结果表明了聚合物 - 药物相容性。获得的H-1 NMR光谱结果表明纳米孔内的药物夹杂物随夹杂物复合物的形成。 XRPD研究表明，负载药物已改变晶体性能改变药物溶解度。 SEM照片揭示了纳米泊的表面上的多孔和海绵状纹理。 Box-Behnken的实验设计是为了优化纳米分子合成。在含有扑热氨基甲醇的合成纳米龙中，考虑了批次F3-P31，F3-A31和F3-C31的批量F3-P31，F3-A31和F3-C31。它们的粒度为185,181和199nm，夹带效率分别为81.53,84.96和89.28％。将这些优化的纳米龙被直接压制成片剂，并研究了预先压缩性质和后压缩性质，包括vitrodrug释放。与纯药物相比，制备的片剂表现出所需的药物溶解特性。上述结果表明纳米龙的适用性在调节药物释放时用不同溶解性进行组合治疗。

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  • 来源
    《RSC Advances》 |2020年第57期|共16页
  • 作者

    Moin Afrasim; Roohi N. K. Famna; Rizvi Syed Mohd Danish; Ashraf Syed Amir; Siddiqui Arif Jamal; Patel Mitesh; Ahmed S. M.; Gowda D. V; Adnan Mohd;

  • 作者单位

    Univ Hail Coll Pharm Dept Pharmaceut POB 2440 Hail Saudi Arabia;

    JSS Acad Higher Educ &

    Res JSS Coll Pharm Dept Pharmaceut Mysuru 570015 Karnataka India;

    Univ Hail Coll Pharm Dept Pharmaceut POB 2440 Hail Saudi Arabia;

    Univ Hail Coll Appl Med Sci Dept Clin Nutr POB 2440 Hail Saudi Arabia;

    Univ Hail Coll Sci Dept Biol POB 2440 Hail Saudi Arabia;

    Veer Narmad South Gujarat Univ Bapalal Vaidya Bot Res Ctr Dept Biosci Surat Gujarat India;

    Juggat Pharma Mysore Rd Bengaluru 560074 Karnataka India;

    JSS Acad Higher Educ &

    Res JSS Coll Pharm Dept Pharmaceut Mysuru 570015 Karnataka India;

    Univ Hail Coll Sci Dept Biol POB 2440 Hail Saudi Arabia;

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  • 正文语种 eng
  • 中图分类 化学;
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