Formulation and evaluation of Fluconazole Nanosuspensions: In vitro characterization and transcorneal permeability studies

被引：4

作者：

Aldosari, Basmah N. ^{[1
]}

Ibrahim, Mohamed Abbas ^{[1
]}

Alqahtani, Yara ^{[1
]}

Abou El Ela, Amal El Sayeh F. ^{[1
]}

机构：

[1] King Saud Univ, Coll Pharm, Dept Pharmaceut, Riyadh 11495, Saudi Arabia

来源：

SAUDI PHARMACEUTICAL JOURNAL | 2024年 / 32卷 / 07期

关键词：

Fluconazole; Nanosuspensions; Solvent evaporation; Stabilizers; Corneal permeation; DRUG-DELIVERY; NANOPARTICLES; SUSPENSIONS; GEL; POLYMER; IRON;

D O I：

10.1016/j.jsps.2024.102104

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The aim in this study was to develop and evaluate a nanofluconazole (FLZ) formulation with increased solubility and permeation rate using nanosuspensions. The FLZ nanosuspensions were stabilized using a variety of stabilizing agents and surfactants in various concentrations. The FLZ nanosuspension was characterized in vitro using particle size, zeta potential, X-ray powder diffraction (XRPD), and solubility. In addition, the ex vivo ocular permeation of FLZ through a goat cornea was analyzed. The results showed that the particle size of all nanosuspension formulations was in the nanometer range from 174.5 +/- 1.9 to 720.2 +/- 4.77 nm; that of the untreated drug was 18.34 mu m. The zeta potential values were acceptable, which indicated suitable stability for formulations. The solubility of the nanosuspensions was up to 5.7-fold higher compared with that of the untreated drug. The results of the ex vivo ocular diffusion of the FLZ nanosuspensions showed the percentage of FLZ penetrating via the goat cornea increased after using Kollicoat to stabilize the nanosuspension formulation. Consequently, when using a nanosuspension formulation of Kollicoat, the antifungal activity of the drug strengthens.

引用

页数：7

共 31 条

[1] Hydrogel Containing PEG-Coated Fluconazole Nanoparticles with Enhanced Solubility and Antifungal Activity [J].

Abdellatif, Ahmed A. H. ;

El-Telbany, Dalia Farag A. ;

Zayed, Gamal ;

Al-Sawahli, Majid M. .

JOURNAL OF PHARMACEUTICAL INNOVATION, 2019, 14 (02) :112-122

[2] Fluconazole nanoparticles prepared by antisolvent precipitation technique: Physicochemical, in vitro, ex vivo and in vivo ocular evaluation [J].

Abou El Ela, Amal El Sayeh F. ;

Ibrahim, Mohamed Abbas ;

Alqahtani, Yara ;

Almomen, Aliyah ;

Aleanizy, Fadilah Sfouq .

SAUDI PHARMACEUTICAL JOURNAL, 2021, 29 (06) :576-585

[3] Co-stabilization of pioglitazone HCL nanoparticles prepared by planetary ball milling: in-vitro and in-vivo evaluation [J].

Alshora, Doaa H. ;

Alsaif, Shaikha ;

Ibrahim, Mohamed A. ;

Ezzeldin, Essam ;

Almeanazel, Osaid T. ;

Abou El Ela, Amal El Sayeh ;

Ashri, Lubna Y. .

PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, 2020, 25 (07) :845-854

[4] Rosuvastatin calcium nanoparticles: Improving bioavailability by formulation and stabilization codesign [J].

Alshora, Doaa H. ;

Ibrahim, Mohamed A. ;

Elzayat, Ehab ;

Almeanazel, Osaid T. ;

Alanazi, Fars .

PLOS ONE, 2018, 13 (07)

[5]

Chen XX, 2009, DRUG DEV IND PHARM, V35, P283, DOI [10.1080/03639040802282896, 10.1080/03639040802282896 ]

[6]

Chowdary K., 2005, INDIAN DRUGS BOMBAY, V42, P557

[7] Rheological characterization of xanthan suspensions of nanoscale iron for injection in porous media [J].

Comba, Silvia ;

Dalmazzo, Davide ;

Santagata, Ezio ;

Sethi, Rajandrea .

JOURNAL OF HAZARDOUS MATERIALS, 2011, 185 (2-3) :598-605

[8] Stabilization of highly concentrated suspensions of iron nanoparticles using shear-thinning gels of xanthan gum [J].

Comba, Silvia ;

Sethi, Rajandrea .

WATER RESEARCH, 2009, 43 (15) :3717-3726

[9] Chitosan nanoparticles:: a new vehicle for the improvement of the delivery of drugs to the ocular surface.: Application to cyclosporin A [J].

De Campos, AM ;

Sánchez, A ;

Alonso, MJ .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 224 (1-2) :159-168

[10]

Esfandi E, 2014, IRAN J PHARM RES, V13, P809

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