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  1. Quantification of atovaquone from amorphous solid dispersion formulation using HPLC: An in vitro and ex vivo investigation
    Teoh XY, Goh CF, Aminu N, Chan SY
    J Pharm Biomed Anal, 2021 Jan 05;192:113631.
    PMID: 33011581 DOI: 10.1016/j.jpba.2020.113631
    Atovaquone (ATQ) is a poorly soluble drug. Therefore, formulating ATQ into its supersaturated state through solid dispersion for bioavailability enhancement can be of great value. However, due to fast crystallising properties of ATQ, the quantification of ATQ in a supersaturated solid dispersion system can be complicated. Therefore, in pursuit of accurate quantification of such sample, a simple HPLC analytical method utilising a C18 column (250 × 4.6 mm ID, 5 μm) for the quantitation of ATQ has been developed and validated. Atovaquone elution using the proposed method demonstrated a retention time around 7.6 min with good linearity (R2 > 0.999). The system suitability is also detailed with the tailing factor at 1.365 ± 0.002. The addition of solubilising agent as sample treatment step aided in ensuring the accurate quantitation of the fast crystallising ATQ. The developed HPLC quantitation method has been successfully employed in the analysis of ATQ from solid dispersion samples in in vitro dissolution as well as ex vivo permeation studies for formulation development.
    Matched MeSH terms: Atovaquone
  2. Solid Lipid Nanoparticles of Atovaquone Based on 2(4) Full-Factorial Design
    Mohtar N, A K Khan N, Darwis Y
    Iran J Pharm Res, 2015;14(4):989-1000.
    PMID: 26664366
    Solid lipid nanoparticles of atovaquone (ATQ-SLN) were prepared by high shear homogenization method using tripalmitin, trilaurin, and Compritol 888 ATO as the lipid matrices and Phospholipon 90H, Tween 80, and poloxamer 188 as the surfactants. Optimization of the formulations was conducted using 6 sets of 2(4) full-factorial design based on four independent variables that were the number of homogenizing cycles, concentration of the lipid, concentration of the co-surfactant, and concentration of the main surfactant. The dependent variables were particle size and polydispersity index (PdI). The homogenizing cycles showed a negative influence on the dependent variables which reduced both the particle size and the PdI value. Moreover, a combination of certain percentages of the main surfactant and co-surfactant also showed a negative influence that reduced both the particle size and PdI value. Selected formulations from each design were further characterized for the entrapment efficiency and yield. The optimised formulation of ATQ-SLN consisted of trilaurin, Phospholipon 90H and Tween 80 with a particle size of 89.4 ± 0.2 nm and entrapment efficiency of 83.0 ± 1.7%. The in-vitro release evaluation of the formulation showed a complete and immediate release of ATQ from the SLN that could be a solution to improve the poor aqueous solubility and hence poor bioavailability of the drug.
    Matched MeSH terms: Atovaquone
  3. Sustainable Dissolution Performance of a Carrier Tailored Electrospun
    Teoh XY, Yeoh Y, Yoong LK, Chan SY
    Pharm Res, 2020 Jan 07;37(2):28.
    PMID: 31912250 DOI: 10.1007/s11095-019-2734-0
    PURPOSE: This study aims to conduct an impact investigation in the hydrophobic-hydrophilic balance as an important factor for dissolution improvement of a hydrophilic carrier-based solid dispersion system.

    METHODS: Polymeric carriers with different hydrophobic to hydrophilic ratios were used to prepare several electrospun solid dispersion formulations. Physicochemical properties and surface morphology of the samples were assessed using Attenuated Total Reflectance Fourier Transform Infrared (ATR-FTIR), polarized light microscopy, Differential Scanning Calorimetry (DSC), X-ray Powder Diffraction (XRPD) and Scanning Electron Microscopy (SEM). Dissolution study was conducted in a non-sink condition to assess the drug release.

    RESULTS: Incorporation of a higher amount of hydrophilic component showed an improvement in formulating a fully amorphous system based on XRPD, yet the dissolution rate increment showed no significant difference from the lower. Hence, the degree of crystallinity is proven not to be the crucial factor contributing to dissolution rate improvement. The presence of a concomitant hydrophobic component, however, showed ability in resisting precipitation and sustaining supersaturation.

    CONCLUSION: Hydrophobicity in a binary carrier system plays an important role in achieving and maintaining the supersaturated state particularly for an amorphous solid dispersion. Graphical Abstract.

    Matched MeSH terms: Atovaquone/chemistry*
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