Department of Pharmacy, University of Malakand, Chakdara, Dir (L), 18800, Khyber Pakhtunkhwa, Pakistan.
Department of Pharmaceutical Sciences, College of Pharmacy-Boys, Al-Dawadmi Campus, Shaqra University, Shaqra, 15572, KSA.
J Biomed Nanotechnol. 2022 Apr 1;18(4):1215-1226. doi: 10.1166/jbn.2022.3313.
Cefixime; widely employed cephalosporin antibiotic is unfortunately coupled to poor water solubility with resultant low oral bioavailability issues. To solve this problem micro-emulsion technique was used to fabricate binary SLNs using blend of solid and liquid lipids, surfactant as well as co-surfactant. The optimized nano suspension was characterized followed by modification to solidified dosage form. During characterization, optimized nano-suspension (CFX-4) produced particle size 189±2.1 nm with PDI 0.310±0.02 as well as -33.9±2 mV zeta potential. Scanning electron microscopy (SEM) presented nearly identical and spherical shaped particles. Differential scanning calorimetry and X-ray powder diffraction analysis ascertained decrease in drug's crystallinity. release of drug pursued zero-order characteristics and demonstrated non-fickian pattern of diffusion. The freeze dried nano suspension (CFX-4) was transformed to capsule dosage form to perform comparison based studies. evaluation corresponded to 2.20-fold and 2.11-fold enhancement in relative bioavailability of CFX nano-formulation (CFX-4) as well as the prepared capsules respectively in contrast to the commercialized product (Cefiget®). In general; the obtained results substantiated superior oral bioavailability along with sustained pattern of drug release for CFX loaded binary nano particles. Thus, binary SLNs could be employed as a resourceful drug carrier for oral CFX delivery.
头孢克肟；一种广泛应用的头孢菌素类抗生素，但其水溶性较差，导致口服生物利用度较低。为了解决这个问题，采用微乳液技术制备了二元固体脂质纳米粒（SLNs），使用了固液混合脂质、表面活性剂和助表面活性剂。对优化的纳米混悬液进行了特征描述，随后对其进行了固化剂型的修饰。在特征描述过程中，优化的纳米混悬液（CFX-4）的粒径为 189±2.1nm，PDI 为 0.310±0.02，ζ 电位为-33.9±2mV。扫描电子显微镜（SEM）显示出几乎相同的、球形的颗粒。差示扫描量热法和 X 射线粉末衍射分析证实了药物结晶度的降低。药物的释放遵循零级特征，并表现出非菲克扩散模式。将冻干的纳米混悬液（CFX-4）转化为胶囊剂型，进行基于研究的比较。评价结果表明，CFX 纳米制剂（CFX-4）和制备的胶囊的相对生物利用度分别提高了 2.20 倍和 2.11 倍，而与商业化产品（Cefiget®）相比。总的来说，研究结果证实了 CFX 负载的二元纳米颗粒具有优越的口服生物利用度和持续的药物释放模式。因此，二元 SLNs 可以作为口服 CFX 给药的有前途的药物载体。
