PEGylated liposome containing sildenafil for the treatment of hypertension
Abstract
The purpose of this study was to prepare PEGylated liposomes containing sildenafil for the treatment of pulmonary arterial hypertension. PEGylated liposomes were prepared by thin film hydration method by varying the concentration of lipids. The prepared liposomes were characterized for the particle size, PDI, zeta potential, % entrapment efficiency and in-vitro release study. The optimized formulation exhibits a particle size of 104.27±1.4 nm, PDI of 0.449±0.02, zeta potential of -42.9±0.7 along with the maximum encapsulation of drug i.e. 87.30±2.6. Optimized formulation showed % cumulative drug release of 85.38±0.26 in 48 hr. From the study it can be concluded that the PEGylated liposomes containing sildenafil for the treatment of pulmonary arterial hypertension provides a sustained release of drug and further studies are required to confirm their efficacy at clinical level.
Keywords: Sildenafil; PEGylated liposomes; Pulmonary arterial hypertension; % entrapment efficiency
Downloads
References
2. Dupuis J, Hoeper M M,. Endothelin receptor antagonists in pulmonary arterial hypertension. Eur. Respir. J. 2008; 31:407–415.
3. Ghasemian E, Vatanara A, Rouini MR, Najafabadi AR, Gilani K, Lavasani H, Mohajel N. Inhaled sildenafil nanocomposites: lung accumulation and pulmonary pharmacokinetics. Pharm Dev Technol, 2015; 1-11.
4. Atyabi F. Dinarvand R, Preparation of PEGylated nano liposomal formulation containing SN-38: in vitro characterization and in vivo biodistribution in mice. Acta Pharmaceutica 2009; 59:133-144.
5. Shavi GV, Reddy MS, Raghavendra R, Dave V, Kushwaha K. PEGylated liposomes of anastrozole for long-term treatment of breast cancer: in-vitro and in-vivo evaluation. J Liposome Res: 2015; 1-9.
6. Maalej CJ, Charcosset C, Fessi H, A new method for liposome preparation using a membrane contactor. J Lipo Res 2011; 21:213–220.
7. Dmitry V, Schaaf P, Mohwald H, Effective embedding of liposomes into polyelectrolyte multilayered films: the relative importance of lipid-polyelectrolyte and inter polyelectrolyte interactions. RSC Adv 2009; 5:1394–1405.
8. Makino K, Yamada T, Kimura M et al, Temperature- and ionic strength-induced conformational changes in the lipid head group region of liposomes as suggested by zeta potential data. Biophy Chem 1991; 41:175–183
9. Betageri GV, Parsons DL Drug encapsulation and release from multilamellar and unilamellar liposomes.Int J Pharm 1992; 81:235–241.
10. Dave V, Sharma S, Yadav RB, Agarwal U. Herbal liposome for the topical delivery of ketoconazole for the effective treatment of seborrheic dermatitis. Appl Nanosci. 2017; 8:973-87.
11. Y Er, Barnes TJ, Fornasiero D, Fornasiero CA, The encapsulation and release of guanosine from PEGylated liposomes. J Liposome Res 2009; 19:29–36.
12. Sezer AD, Bas AL, Akbuga J, Encapsulation of enrofloxacin in liposomes: preparation and in-vitro characterization. J Liposome Res 2004; 14(1&2):77–86.
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License. that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).
.