Inclusion complexes between sildenafil citrate and cyclodextrins enhance drug solubility

Atipairin, Apichart; Sawatdee, Somchai

doi:10.1016/j.ajps.2015.11.105

Cited by 11 publications

(8 citation statements)

References 3 publications

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“…Generally, drugs should be sufficiently hydrophobic in order to penetrate biological membranes via passive diffusion, but at the same time possess some hydrophilicity in aqueous medium. For many pharmaceutical applications, it was shown that inclusion complex helped to improve solubility (Aiassa et al, 2015; Atipairin, Sawatdee, 2016; Freitas et al, 2012;Ol'khovich et al, 2014;Priya et al, 2013;Shende et al, 2015;Zhang et al, 2013a;Zhang et al, 2013b;Franco et al, 2009;Ruan et al, 2005;Tang et al, 2015;De Araujo et al, 2008), stability (Freitas et al, 2012;Shende et al, 2015;Kicuntod et al, 2016), bioavailability (Atipairin, Sawatdee, 2016;Zhang et al, 2013a), and therapeutic effect (Zhang et al, 2013b), between various drugs and cyclodextrins. Inclusion complexes of epothilone (Xiao et al, 2014), oxaliplatin (Zhang et al, 2016), paclitaxel (Hamada et al, 2006), etc.…”

Section: Introductionmentioning

confidence: 99%

Complexation and enhancement of temozolomide solubility with cyclodextrins

Gurten

Yenigül

Sezer

et al. 2018

Braz. J. Pharm. Sci.

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Temozolomide is a poorly soluble anti-cancer drug used in the treatment of some brain cancers. Following literature reports about the enhancement of solubility and stability for these kinds of drugs upon complexation with cyclodextrins, we aimed to form an inclusion complex between temozolomide and the different types of cyclodextrins (CDs) to enhance its solubility. In this study, three different cyclodextrins (β-CD, hydroxyl-β-CD and γ-CD) were used, and changes in solubility was measured by UV-Vis Spectroscopy and HPLC. Morphological changes upon complexation were shown by the Scanning Electron Microscope (SEM), and weight loss profiles with respect to temperatures which were unique to the compounds were shown by Thermogravimetric Analysis. Changes in heat release profiles were shown by Differential Scanning Calorimeter (DSC). Drug solubility was measured to be increased to around 25% for 1:1 molar ratio for all used CD complexations. Changes of morphology, heat release and weight loss profiles are consistent with the formation of an inclusion complex between CDs and temozolomide. In this study, success was shown in the enhancement of temozolomide solubility upon complexation with different types of CDs. It has been demonstrated that cyclodextrins can be used as complexing agents for poorly soluble anti-cancer drugs, increasing their solubility and hence drug availability.

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Section: Introductionmentioning

confidence: 99%

Complexation and enhancement of temozolomide solubility with cyclodextrins

Gurten

Yenigül

Sezer

et al. 2018

Braz. J. Pharm. Sci.

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“…As reported in previous studies, sildenafil citrate can form inclusion complexes with α-cyclodextrin via a 1:1 stoichiometric ratio. 6,12,15,16 The solubility of sildenafil increased by raising the concentration of α-cyclodextrin. To obtain 20 µg of sildenafil per inhalation dose, we used 28 µg of a sildenafil citrate salt.…”

Section: Discussionmentioning

confidence: 99%

“…To obtain 20 µg of sildenafil per inhalation dose, we used 28 µg of a sildenafil citrate salt. To promote the 1:1 complex formation of sildenafil and α-cyclodextrin, we used 41 µg of α-cyclodextrin w to complete the inclusion complex with 28 µ with sildenafil citrate 6,12,15,16 The spray-dried complex of sildenafil citrate with α-cyclodextrin was free-flowing and had a spheroidal shape (observed by light microscope) that was suitable for use in DPIs. 17 We chose the Rotahaler ® in this experiment to deliver the dry powder due to its ease of use and high-performance delivery of drugs to the lung.…”

Section: Discussionmentioning

confidence: 99%

“…[6][7][8][9][10][11] There are previously report sildenafil citrate complexed with α-cyclodextrin to enhance the solubility of sildenafil as a linear function of cyclodextrin concentration. 12 The complex of sildenafil citrate and α-cyclodextrin is one-to-one complex formation. 7,12 Currently, there are no reports regarding the formulation of sildenafil complexed with α-cyclodextrin for use in a DPI.…”

Section: Introductionmentioning

confidence: 99%

“…12 The complex of sildenafil citrate and α-cyclodextrin is one-to-one complex formation. 7,12 Currently, there are no reports regarding the formulation of sildenafil complexed with α-cyclodextrin for use in a DPI. Development of sildenafil citrate complexed with α-cyclodextrin is beneficial due to its enhanced solubility in the lung.…”

Section: Introductionmentioning

confidence: 99%

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Development of Spray-Dried Sildenafil Citrate -α-cyclodextrin Complexes for Use in Dry Powder Inhalers

Atipairin

Sawatdee

2020

IJPI

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Background: Sildenafil citrate is a drug used in the treatment of pulmonary hypertension. The development of sildenafil citrate complexed with α-cyclodextrin as dry powder inhaler (DPI) should enhance its solubility in the lung. Methods: Sildenafil citrate was dissolved with α-cyclodextrin solution at pH 4.5 to obtain inclusion complexes. The complex solution was spray-dried to make spheroidal powder. The sildenafil DPI formulations were mixed with coarse lactose and fine lactose as carriers and then filled in capsule no. 2. Three different ratios of course to fine lactose were used (1:1 (#1), 2:1 (#2) and 3:1 (#3)) to optimize the performance and aerosol properties. The fine particle fraction (FPF), mass median aerodynamic diameter (MMAD) and geometric standard deviation (GSD) were used to evaluate the in vitro drug delivery performance in the lung by in vitro. Results: The proportion of sildenafil in formulations #1, #2, #3 was 100.2% ± 0.1%, 100.1% ± 0.2% and 98.9% ± 0.1%, respectively. The aerosol properties of the best formulation (#2) were as follows: an ED of 85.5 ± 0.5%, an FPF of 56.6 ± 2.3%, an MMAD of 3.2 ± 0.6 µm and a GSD of 1.02±0.01. Conclusion: Sildenafil citrate complexed with α-cyclodextrin was successfully developed for a DPI by using coarse and fine lactose monohydrate in a 2:1 ratio.This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms.

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