School of Pharmaceutical and Population Health Informatics (SoPPHI), DIT University, Dehradun, India.
Department of Biology, Faculty of Science, Princess Nourah Bint Abdulrahman University, Riyadh, Saudi Arabia.
Front Public Health. 2023 Dec 27;11:1238961. doi: 10.3389/fpubh.2023.1238961. eCollection 2023.
Berberine-encapsulated polyelectrolyte nanocomposite (BR-PolyET-NC) gel was developed as a long-acting improved wound healing therapy. BR-PolyET-NC was developed using an ionic gelation/complexation method and thereafter loaded into Carbopol gel. Formulation was optimized using Design-Expert® software implementing a three-level, three-factor Box Behnken design (BBD). The concentrations of polymers, namely, chitosan and alginate, and calcium chloride were investigated based on particle size and %EE. Moreover, formulation characterized for biopharmaceutical performances and their wound healing potency was evaluated in adult BALB/c mice. The particle distribution analysis showed a nanocomposite size of 71 ± 3.5 nm, polydispersity index (PDI) of 0.45, ζ-potential of +22 mV, BR entrapment of 91 ± 1.6%, and loading efficiency of 12.5 ± 0.91%. Percentage drug release was recorded as 89.50 ± 6.9% with pH 6.8, thereby simulating the wound microenvironment. The investigation of the nanocomposite gel revealed uniform consistency, well spreadability, and extrudability, which are ideal for topical wound use. The analytical estimation executed using FT-IR, DSC, and X-ray diffraction (XRD) indicated successful formulation with no drug excipients and without the amorphous state. The colony count of microbes was greatly reduced in the BR-PolyET-NC treated group on the 15th day from up to 6 CFU compared to 20 CFU observed in the BR gel treated group. The numbers of monocytes and lymphocytes counts were significantly reduced following healing progression, which reached to a peak level and vanished on the 15th day. The observed experimental characterization and study indicated the effectiveness of the developed BR-PolyET-NC gel toward wound closure and healing process, and it was found that >99% of the wound closed by 15th day, stimulated via various anti-inflammatory and angiogenic factors.
作为一种长效改良的伤口愈合治疗方法，开发了黄连素包埋聚电解质纳米复合材料（BR-PolyET-NC）凝胶。BR-PolyET-NC 是通过离子凝胶/络合方法开发的，然后载入卡波姆凝胶中。使用 Design-Expert®软件实现三水平三因素 Box-Behnken 设计（BBD）优化配方。基于粒径和 EE%研究了聚合物，即壳聚糖和海藻酸钠，以及氯化钙的浓度。此外，对制剂的生物制药性能进行了表征，并在成年 BALB/c 小鼠中评估了其伤口愈合效果。颗粒分布分析显示纳米复合材料的粒径为 71±3.5nm、多分散指数（PDI）为 0.45、Zeta 电位为+22mV、BR 包封率为 91±1.6%、载药量为 12.5±0.91%。在 pH6.8 下，记录到 89.50±6.9%的药物释放率，模拟了伤口微环境。纳米复合凝胶的研究表明，其具有均匀的一致性、良好的铺展性和可挤出性，非常适合局部伤口使用。使用傅里叶变换红外光谱（FT-IR）、差示扫描量热法（DSC）和 X 射线衍射（XRD）进行的分析评估表明，该配方成功地实现了药物赋形剂的负载，且没有药物赋形剂和非晶态。与 BR 凝胶治疗组观察到的 20 CFU 相比，BR-PolyET-NC 治疗组第 15 天的微生物菌落计数大大减少，高达 6 CFU。随着愈合过程的进行，单核细胞和淋巴细胞计数显著减少，在第 15 天达到峰值并消失。观察到的实验特性和研究表明，所开发的 BR-PolyET-NC 凝胶在伤口闭合和愈合过程中具有有效性，并且发现 >99%的伤口在第 15 天通过各种抗炎和血管生成因子愈合。
