Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Int J Pharm. 2012 Oct 15;436(1-2):611-6. doi: 10.1016/j.ijpharm.2012.07.028. Epub 2012 Jul 26.
Amphotericin B (AmB) lipid nanoemulsions were prepared and characterized and their suitability for pulmonary delivery via nebulization was evaluated. AmB nanoemulsions were prepared by sonicating and vortexing the drug with two commercially available lipid nanoemulsions: the Intralipid(®) or Clinoleic(®). Loading the nanoemulsions with the drug slightly increased the size of the lipid droplets and did not affect the zeta potential of the nanoemulsions. The loading efficiency of AmB was found to be 87.46±2.21% in the Intralipid(®) nanoemulsions and 80.7±0.70% in the Clinoleic(®) formulation. This respectively corresponded to 21.86 mg and 20.19 mg of AmB being successfully loaded in the nanoemulsions. On aerosolization using a Pari Sprint jet nebulizer, both nanoemulsions produced very high drug output which was approximately 90% for both formulations. Using the two-stage impinger, the Clinoleic(®) emulsion had higher fine particle fraction (FPF) than the Intralipid(®), since the Clinoleic(®) displayed higher deposition of AmB in the lower impinger stage (exceeding 80%), compared to 57% for the Intralipid(®). Overall, the ease of preparation of the AmB lipid nanoemulsions, along with their in vitro nebulization performance suggest that lipid nanoemulsions could be successful nanocarriers for delivery of AmB to the peripheral respiratory airways.
两性霉素 B(AmB)脂质纳米乳液被制备并进行了表征,评估了其通过雾化用于肺部给药的适用性。AmB 纳米乳液是通过超声处理和涡旋药物与两种市售的脂质纳米乳液:Intralipid(®)或 Clinoleic(®)来制备的。将纳米乳液负载药物会略微增加脂质液滴的大小,但不会影响纳米乳液的 ζ 电位。在 Intralipid(®)纳米乳液中,AmB 的负载效率为 87.46±2.21%,在 Clinoleic(®)制剂中为 80.7±0.70%。这分别对应于 21.86 毫克和 20.19 毫克的 AmB 成功负载在纳米乳液中。使用 Pari Sprint 射流雾化器进行雾化时,两种纳米乳液都产生了非常高的药物输出,两种制剂的输出率均约为 90%。使用两段式冲击器,Clinoleic(®)乳液的细颗粒分数(FPF)高于 Intralipid(®),因为与 Intralipid(®)相比,Clinoleic(®)在下部冲击器阶段显示出更高的 AmB 沉积(超过 80%),而 Intralipid(®)则为 57%。总体而言,两性霉素 B 脂质纳米乳液的制备简便,以及其体外雾化性能表明,脂质纳米乳液可能是将两性霉素 B 递送至周围呼吸道的成功纳米载体。