Jain Ashay, Thakur Deepika, Ghoshal Gargi, Katare O P, Singh Bhupinder, Shivhare U S
Dr. S. S. Bhatnagar University Institute of Chemical Engineering & Technology, Panjab University, Chandigarh, India; Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, UGC-Centre of Advanced Studies, Panjab University, Chandigarh 160 014, India; UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles and Nanocomposites, Panjab University, Chandigarh 160 014, India.
Dr. S. S. Bhatnagar University Institute of Chemical Engineering & Technology, Panjab University, Chandigarh, India.
Int J Biol Macromol. 2016 Dec;93(Pt A):746-756. doi: 10.1016/j.ijbiomac.2016.08.071. Epub 2016 Aug 27.
The current work entails a novel strategy of formulating the microparticles of lycopene solely using rational blends of biopolymers without using equipment-intensive techniques. The study is intended to enhance oral bioavailability of lycopene by controlling its release from micro-formulation and facilitating its absorption though lymphatic pathways. Considering the minimum particle size, maximum entrapment efficiency and loading capacity, the amounts of casein (i.e., protein) and gum tragacanth (i.e., polysaccharide) were selected as the critical factors for formulation of microparticles. Complex formation and electrostatic interaction was confirmed by Fourier transform infra red (FTIR) spectra. Size and surface properties of microparticles were studied using scanning electron microscopy (SEM). The optimized formulation (mean particle size: ∼130μm; % entrapment efficiency: ∼67% and loading capacity: ∼71%) designated noticeable improvement in lycopene release profile (over 80% in 24h). Increment in the values of C (2.22-fold) and AUC (1.97-fold) further indicated noteworthy augmentation in the rate and extent of bioavailability by the microparticles formulation compared to plain lycopene. The resulting formulation was found to be quite stable all through two months of study episode. The resultant microparticles formulation was evaluated for antioxidant activity and tested for their effectiveness in self life enhancement of vegetable oil by calculating peroxide value under temperature and storage condition. Encapsulation strongly increased the stability of micronutrients. The current investigations, therefore, report the successful development of biopolymeric microparticles with improved bioavailability potential of lycopene.
当前的工作需要一种全新的策略,即仅使用生物聚合物的合理混合物来制备番茄红素微粒,而不使用设备密集型技术。该研究旨在通过控制番茄红素从微制剂中的释放并促进其通过淋巴途径的吸收来提高其口服生物利用度。考虑到最小粒径、最大包封率和载药量,选择酪蛋白(即蛋白质)和刺梧桐胶(即多糖)的用量作为制备微粒的关键因素。通过傅里叶变换红外光谱(FTIR)证实了复合物的形成和静电相互作用。使用扫描电子显微镜(SEM)研究了微粒的尺寸和表面性质。优化后的制剂(平均粒径:约130μm;包封率:约67%;载药量:约71%)在番茄红素释放曲线方面有显著改善(24小时内超过80%)。与普通番茄红素相比,微粒制剂的C值(2.22倍)和AUC值(1.97倍)增加,进一步表明其生物利用度的速率和程度有显著提高。在为期两个月的研究期间,发现所得制剂相当稳定。通过在温度和储存条件下计算过氧化值,对所得微粒制剂的抗氧化活性进行了评估,并测试了其在提高植物油保质期方面的有效性。包封大大提高了微量营养素的稳定性。因此,当前的研究报告了具有提高番茄红素生物利用度潜力的生物聚合物微粒的成功开发。