Zafar Ameeduzzafar, Alruwaili Nabil K, Imam Syed Sarim, Yasir Mohd, Alsaidan Omar Awad, Alquraini Ali, Rawaf Alenazy, Alsuwayt Bader, Anwer Md Khalid, Alshehri Sultan, Ghoneim Mohammed M
Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Pharmaceutics. 2022 Feb 25;14(3):507. doi: 10.3390/pharmaceutics14030507.
In the present research study, we formulate bilosomes (BMs) of diclofenac (DC) for oral delivery for enhancement of therapeutic efficacy (anti-inflammatory disease). The BMS were prepared by thin film hydration method and optimized by Box−Behnken design (BBD) using cholesterol (A), lipid (B), surfactant (C), and bile salt (D) as formulation factors. Their effects were evaluated on vesicle size (Y1) and entrapment efficacy (Y2). The optimized DC-BMs-opt showed a vesicle size of 270.21 ± 3.76 nm, PDI of 0.265 ± 0.03, and entrapment efficiency of 79.01 ± 2.54%. DSC study result revealed that DC-BMs-opt exhibited complete entrapment of DC in BM matrix. It also depicted significant enhancement (p < 0.05) in release (91.82 ± 4.65%) as compared to pure DC (36.32 ± 4.23%) and DC-liposomes (74.54 ± 4.76%). A higher apparent permeability coefficient (2.08 × 10−3 cm/s) was also achieved compared to pure DC (6.6 × 10−4 cm/s) and DC-liposomes (1.33 × 10−3 cm/s). A 5.21-fold and 1.43-fold enhancement in relative bioavailability was found relative to pure DC and DC liposomes (DC-LP). The anti-inflammatory activity result showed a significant (p < 0.05) reduction of paw edema swelling compared to pure DC and DC-LP. Our findings revealed that encapsulation of DC in BMs matrix is a good alternative for improvement of therapeutic efficacy.
在本研究中，我们制备了用于口服给药的双氯芬酸（DC）双分子层脂质体（BMs），以提高治疗效果（抗炎疾病）。通过薄膜水化法制备双分子层脂质体，并使用胆固醇（A）、脂质（B）、表面活性剂（C）和胆盐（D）作为制剂因素，通过Box-Behnken设计（BBD）进行优化。评估它们对囊泡大小（Y1）和包封率（Y2）的影响。优化后的DC-BMs-opt囊泡大小为270.21±3.76nm，多分散指数（PDI）为0.265±0.03，包封效率为79.01±2.54%。差示扫描量热法（DSC）研究结果表明，DC-BMs-opt中DC完全包封在双分子层脂质体基质中。与纯DC（36.32±4.23%）和DC脂质体（74.54±4.76%）相比，它还显示出释放率显著提高（p<0.05）（91.82±4.65%）。与纯DC（6.6×10−4cm/s）和DC脂质体（1.33×10−3cm/s）相比，还获得了更高的表观渗透系数（2.08×10−3cm/s）。相对于纯DC和DC脂质体（DC-LP），相对生物利用度提高了5.21倍和1.43倍。抗炎活性结果表明，与纯DC和DC-LP相比，爪部水肿肿胀显著（p<0.05）减轻。我们的研究结果表明，将DC包封在双分子层脂质体基质中是提高治疗效果的一个良好选择。
