Preparation and Evaluation of Inhalable Sustained Release Sildenafil Citrate Solid Lipid Microparticles Dispersions
Keywords:
sildenafil citrate, glyceryl behenate, closed melt method, solid lipid microparticles dispersions, dry powder inhaler
Abstract
This is a preliminary study utilizing drug targeting approach for developing sildenafil citrate (SFC) pulmonary delivery system, a first -line for pulmonary arterial hypertension (PAH) treatment and hence reducing the dose and the side effects. The closed melt method was employed for preparing SFC -solid lipid microparticles dispersions (SFC -SLMDs), a nonsolvent technique aid in the production of drug -matrix dispersions with sustained release properties. Glyceryl behenate (GB) (Compritol® 888 ATO) was used as the retarding matrix and the results shown that as its ratio increase there was a decrease in the fine particle fraction, an increase in the drug content and a prolong drug release pattern. The best model fit the release data was Higuchi -Matrix model which indicates drug diffusion -controlled releasing mechanism. Thus, inhaled SFC -SLMDs dry powder will improve PAH treatment via drug localization at low doses and reducing the administration frequency.
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References
Lyn Frumkin (2012) The Pharmacological Treatment of Pulmonary Arterial Hypertension. 64(3), 583-620.
M -C Chaumais, S Perrin, O Sitbon, G Simonneau, M Humbert, D Montani (2013) Pharmacokinetic Evaluation of Sildenafil as a Pulmonary Hypertension Treatment. 9(9), 1193-1205.
N Labiris, M Dolovich (2003) Pulmonary drug delivery. Part I: Physiological factors affecting therapeutic effectiveness of aerosolized medications. 56(6), 588-599.
M Beck -Broichsitter, P Kleimann, T Gessler, W Seeger, T Kissel, T Schmehl (2012) Nebulization Performance of Biodegradable Sildenafil -Loaded Nanoparticles using the Aeroneb ® Pro: Formulation Aspects and Nanoparticle Stability to Nebulization. 422(1 -2), 398-408.
Mukta Paranjpe, Christel Müller-Goymann (2014) Nanoparticle-Mediated Pulmonary Drug Delivery: A Review. 15(4), 5852-5873.
M Paranjpe, V Neuhaus, J Finke, C Richter, T Gothsch, A Kwade, S Buttgenbach, A Braun, C Muller -Goymann (2013) In Vitro and Ex Vivo Toxicological Testing of Sildenafil -Loaded Solid Lipid Nanoparticles. 25(9), 536-543.
Somchai Sawatdee, Hirihattaya Phetmung, Teerapol Srichana (2013) Sildenafil citrate monohydrate-cyclodextrin nanosuspension complexes for use in metered-dose inhalers. 455(1-2), 248-258.
David Cipolla, Boris Shekunov, Jim Blanchard, Anthony Hickey (2014) Lipid-based carriers for pulmonary products: Preclinical development and case studies in humans. 75, 53-80.
Ysr Elnaggar, M El-Massik, O Abdallah (2011) Fabrication, Appraisal, and Transdermal Permeation of Sildenafil Citrate-Loaded Nanostructured Lipid Carriers versus Solid Lipid Nanoparticles. 6, 3195-3205.
S Jagdale, S Patil, B Kuchekar, A Chabukswar (2011) Preparation and Characterization of Metformin Hydrochloride − Compritol 888 ATO Solid Dispersion. 3(3), 197-204.
Michael Tsifansky, Yoon Yeo, Oleg Evgenov, Evangelia Bellas, John Benjamin, Daniel Kohane (2008) Microparticles for Inhalational Delivery of Antipseudomonal Antibiotics. 10(2), 254-260.
Adamo Fini, Cristina Cavallari, Francesca Ospitali, M Gonzalez-Rodriguez (2011) Theophylline-Loaded Compritol Microspheres Prepared by Ultrasound-Assisted Atomization. 100(2), 743-757.
Zahra Daman, Kambiz Gilani, Abdolhossein Rouholamini Najafabadi, Hamid Eftekhari, Mohammad Barghi (2014) Formulation of inhalable lipid-based salbutamol sulfate microparticles by spray drying technique. 22(1).
Tarek Ahmed (2014) Preparation of transfersomes encapsulating sildenafil aimed for transdermal drug delivery: Plackett-Burman design and characterization. 25(1), 1-10.
Matteo Mezzena, Santo Scalia, Paul Young, Daniela Traini (2009) Solid Lipid Budesonide Microparticles for Controlled Release Inhalation Therapy. 11(4), 771-778.
Nispa Seetapan, Piyawan Bejrapha, Wanwisa Srinuanchai, Satit Puttipipatkhachorn, Uracha Ruktanonchai (2010) Nondestructive rheological measurement of aqueous dispersions of solid lipid nanoparticles: effects of lipid types and concentrations on dispersion consistency. 36(9), 1005-1015.
M Üner, G Yener (2007) Importance of Solid Lipid Nanoparticles (SLN) in Various Administration Routes and Future Perspectives. 2(3), 289-300.
Abdul Qadir, M Rahman, M Karim, M Akter, S, Bin Awkat, T, Reza Ms (2003) Evaluation of Hydrophobic Materials as Matrices for Controlled -Release Drug Delivery. 16(2), 17-28.
Yong Zhang, Meirong Huo, Jianping Zhou, Aifeng Zou, Weize Li, Chengli Yao, Shaofei Xie (2010) DDSolver: An Add-In Program for Modeling and Comparison of Drug Dissolution Profiles. 12(3), 263-271.
S Dash, P Murthy, L Nath, P Chowdhury (2010) Kinetic Modeling on Drug Release from Controlled Drug Delivery Systems. 67(3), 217-223.
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2014-10-25
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