Preparation and in vitro release of sildenafil citrate loaded nanostructured lipid carrier

Published on Jul. 29, 2023Total Views: 564 times Total Downloads: 135 times Download Mobile

Author: Ze-Rong LI ¹ Zhao-Li WU ² Wen-Mei QIAO ³  Jing-Ling TANG ²

Affiliation: 1. Shenzhen Second People’s Hospital (The First Affiliated Hospital of Shenzhen University), Shenzhen 518025, Guangdong Province, China 2. College of Pharmacy, Harbin Medical University, Harbin 150076, China 3. Shenzhen Third People's Hospital (The Second Affiliated Hospital of South University of Science and Technology), Shenzhen 518112, Guangdong Province, China

Keywords: Sildenafil citrate Nanostructured lipid carriers Thin film ultrasonic dispersion method In vitro release

DOI: 10.19960/j.issn.1005-0698.202307007

Reference: Ze-Rong LI, Zhao-Li WU, Wen-Mei QIAO, Jing-Ling TANG.Preparation and in vitro release of sildenafil citrate loaded nanostructured lipid carrier[J].Yaowu Liuxingbingxue Zazhi,2023, 32(7): 774-779.DOI: 10.19960/j.issn.1005-0698.202307007.[Article in Chinese]  Copied

Abstract
Full-text
References

Abstract

Objective To prepare sildenafil citrate loaded nanostructured lipid carriers (SC-NLCs), characterize their physical and chemical properties, and evaluate their in vitro release.

Methods SC-NLCs were prepared by thin film ultrasonic dispersion method, and their physical and chemical properties were investigated. The content of sildenafil citrate in SC-NLCs released in vitro was determinated by HPLC. The release properties of SC-NLCs and sildenafil citrate solution in vitro were investigated by dynamic membrane dialysis.

Results SC-NLCs were dispersed in water as milky white and visible colloidal solution and had good dispersion characteristics. The transmission electron microscope observation showed that SC-NLCs were relatively round and evenly distributed. The average particle size, encapsulation efficiency, potential and polydispersity coefficient of SC-NLCs were 66.96 nm, (69.26±0.73)%, (18.00±4.84) mV and 0.247, respectively. The results of in vitro release test showed that the cumulative release of sildenafil citrate in the sildenafil citrate solution group was reached (97.32±3.14)% after 4 hours in PBS (pH 5.5), while the cumulative release of sildenafil citrate in the SC-NLCs group was about (72.16±2.51)% after 4 hours, then reaching the release platform after 24 hours with the cumulative release of (84.29±2.00)%.

Conclusion The prepared SC-NLCs have uniform particle size and uniform dispersion. In terms of in vitro release behavior, SC-NLCs also have good sustained-release properties.

Full-text

Please download the PDF version to read the full text: download

References

1.Mohamed NA, Abou-Saleh H, Kameno Y, et al. Studies on metal-organic framework (MOF) nanomedicine preparations of sildenafil for the future treatment of pulmonary arterial hypertension[J]. Sci Rep, 2021, 11(1): 4336. DOI: 10.1038/s41598-021-83423-6.

2.Nguyen TT, Yi EJ, Hwang KM, et al. Formulation and evaluation of carrier-free dry powder inhaler containing sildenafil[J]. Drug Deliv Transl Re, 2019, 9(1): 319-333. DOI: 10.1007/s13346-018-0586-5.

3.Shahin H, Vinjamuri BP, Mahmoud AA, et al. Formulation and optimization of sildenafil citrate-loaded PLGA large porous microparticles using spray freeze-drying technique: a factorial design and in-vivo pharmacokinetic study[J]. Int J Pharm, 2021, 597: 120320. DOI: 10.1016/j.ijpharm.2021.120320.

4.Rashid J, Patel B, Nozik-Grayck E, et al. Inhaled sildenafil as an alternative to oral sildenafil in the treatment of pulmonary arterial hypertension (PAH)[J]. J Control Release, 2017, 250: 96-106. DOI: 10.1016/j.jconrel.2017.02.003.

5.Shahin HI, Vinjamuri BP, Mahmoud AA, et al. Design and evaluation of novel inhalable sildenafil citrate spray-dried microparticles for pulmonary arterial hypertension[J]. J Control Release, 2019, 302: 126-139. DOI: 10.1016/j.jconrel.2019.03.029.

6.Zauner W, Farrow NA, Haines AM. In vitro uptake of polystyrene microspheres: effect of particle size, cell line and cell density[J]. J Control Release, 2001, 71(1): 39-51. DOI: 10.1016/s0168-3659(00)00358-8.

7.Sharma G, Thakur K, Raza K, et al. Nanostructured lipid carriers: a new paradigm in topical delivery for dermal and transdermal applications[J]. Crit Rev Ther Drug Carrier Syst, 2017, 34(4):355-386. DOI: 10.1615/CritRevTherDrugCarrierSyst.2017019047.

8.Mohammadi M, Pezeshki A, Mesgari AM, et al. Vitamin D3-loaded nanostructured lipid carriers as a potential approach for fortifying food beverages; in vitro and in vivo evaluation[J]. Adv Pharm Bull, 2017, 7(1): 61-71. DOI: 10.15171/apb.2017.008.

9.Weber S, Zimmer A, Pardeike J. Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) for pulmonary application: a review of the state of the art[J]. Eur J Pharm Biopharm, 2014, 86(1): 7-22. DOI: 10.1016/j.ejpb.2013.08.013.

10.王岚, 刘颖, 冯年平. 脂质纳米粒给药系统体外释放方法研究进展[J]. 中国实验方剂学杂志, 2013, 19(18): 350-356. [Wang L, Liu Y, Feng NP. Development of in vitro release methods in lipid nanoparticles drug delivery system[J]. Chinese Journal of Experimental Traditional Medical Formulae, 2013, 19(18): 350-356.] DOI: 10.11653/syfj2013180350.

11.D'Souza SS, DeLuca PP. Methods to assess in vitro drug release from injectable polymeric particulate systems[J]. Pharm Res, 2006, 23(3): 460-474. DOI: 10.1007/s11095-005-9397-8.