Lipid nanocarriers for tamoxifen citrate/coenzyme Q10 dual delivery

El-Leithy, Eman S.; Abdel-Rashid, Rania S.

doi:10.1016/j.jddst.2017.07.020

“…It could be concluded that LNCs reached the dermis, while PNCs were more retained at the outermost layers of the skin. The result was in accordance with the flexibility in a way that higher flexibility gives deeper penetration and high compatibility of phosphatidylcholine in LNCs with skin composition (Coverdale et al., 2017 ; El-Leithy & Abdel-Rashid, 2017 ). Based on retentivity results as shown in Figure 7 , it was found that F1 (PNCs optimum formula) showed more amount drug deposition compared to F6 (LNCs optimum formula).…”

Section: Resultssupporting

confidence: 75%

Polymeric versus lipid nanocapsules for miconazole nitrate enhanced topical delivery: in vitro and ex vivo evaluation

Abdel-Rashid

¹

,

Helal

²

,

Alaa-Eldin

³

et al. 2022

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Nanocapsules can be equated to other nanovesicular systems in which a drug is entrapped in a void containing liquid core surrounded by a coat. The objective of the present study was to investigate the potential of polymeric and lipid nanocapsules (LNCs) as innovative carrier systems for miconazole nitrate (MN) topical delivery. Polymeric nanocapsules and LNCs were prepared using emulsification/nanoprecipitation technique where the effect of poly(ε-caprolactone (PCL) and lipid matrix concentrations with respect to MN were assessed. The resulted nanocapsules were examined for their average particle size, zeta potential, %EE, and in vitro drug release. Optimum formulation in both polymeric and lipidic nanocapsules was further subjected to anti-fungal activity and ex vivo permeation tests. Based on the previous results, nanoencapsulation strategy into polymeric and LNCs created formulations of MN with slow biphasic release, high %EE, and improved stability, representing a good approach for the delivery of MN. PNCs were best fitted to Higuchi’s diffusion while LNCs followed Baker and Lonsdale model in release kinetics. The encapsulated MN either in PNCs or LNCs showed higher cell viability in WISH amniotic cells in comparison with free MN. PNCs showed less ex vivo permeation. PNCs were accompanied by high stability and more amount drug deposition (32.2 ± 3.52 µg/cm 2 ) than LNCs (12.7 ± 1.52 µg/cm 2 ). The antifungal activity of the PNCs was high 19.07 mm compared to 11.4 mm for LNCs. In conclusion, PNCs may have an advantage over LNCs by offering dual action for both superficial and deep fungal infections.

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“…On the other hand soluplus, showed well-defined characteristic peaks which are; 3439 cm -1 for (OH) stretching group, 2932 cm -1 for aromatic (CH) stretching group, 1736 cm -1 and 1638 cm -1 for carbonyl stretching group and 1478 cm-1 for (C-O-C) stretching group.The solid dispersion showed a shifting (OH) stretching group to 3460 cm-1 due to a possible hydrogen bonding [20,14]. The solid dispersion showed a shifting (OH) stretching to 3460/cm due to possible hydrogen bonding [5,14] (Fig. 3).…”

Section: Ftirmentioning

confidence: 91%

Enhancement of the Solubility and the Dissolution Rate of Tamoxifen Citrate Solid Dispersion Using Soluplus by Solvent Evaporation Technique

Abduljabbar

¹

,

Alhammid

²

2019

Asian J Pharm Clin Res

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Objective: The aim of the present study was the enhancement in the solubility of tamoxifen citrate using solid dispersion which is considered as a great solution to overcome the poor water solubility behavior of tamoxifen citrate (TMX) by solvent evaporation technique using Soluplus® as a novel carrier then formulate it as an orodispersible tablet.Method: A total of 24 formulas were prepared as a solid dispersion by solvent evaporation method using Soluplus® as a polymeric solubilizer in the ratio of 1:1, 1:3, 1:5, 1:7, and 1:10 then formulated as orodispersible tablets by incorporating three types of superdisintegrants; croscarmellose, crospovidone, and sodium starch glycolate (SSG) with the solid dispersion. Characterization of the formulation was done using differential scanning colorimetry, Fourier transforms infrared spectroscopy, X-ray diffraction, and scanning electron microscope and the best formula was selected according to the disintegration and dissolution tests.Results and Discussion: Formula 22 were selected as the best formula which contains mixed types of superdisintegrants; croscarmellose and SSG with the fastest complete disintegration of 6.5 s and complete dissolution with <2 min.Conclusion: Accordingly, TMX was successfully enhanced its water solubility by converting its crystalline structure into the amorphous state through solid dispersion with Soluplus® and formulated as an orodispersible tablet to improve its oral absorption.

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“…On the other hand soluplus, showed well-defined characteristic peaks Abduljabbar and Alhammid which are; 3439 cm -1 for (OH) stretching group, 2932 cm -1 for aromatic (CH) stretching group, 1736 cm -1 and 1638 cm -1 for carbonyl stretching group and 1478 cm-1 for (C-O-C) stretching group.The solid dispersion showed a shifting (OH) stretching group to 3460 cm-1 due to a possible hydrogen bonding [20,14]. The solid dispersion showed a shifting (OH) stretching to 3460/cm due to possible hydrogen bonding [5,14] (Fig. 3).…”

Section: Ftirmentioning

confidence: 91%

“…On oral administration, only a limited amount of TMX is absorbed and reaches the blood circulation due to the low water solubility and an extensive first-pass metabolism [4,5]. Accordingly, there are numerous approaches attempted to overcome those obstacles one of them is by improving their water solubility through a nano sizing method or incorporation with coenzymes to avoid enzymatic degradation by the liver [5]. Solid dispersion is one of the approaches that used to improve the solubility of slightly soluble drugs like tamoxifen citrate since solid dispersion has many advantages like simplicity and low cost [6].…”

Section: Introductionmentioning

confidence: 99%

Enhancement of the Solubility and the Dissolution Rate of Tamoxifen Citrate Solid Dispersion Using Soluplus by Solvent Evaporation Technique

Abduljabbar¹,

Alhammid²

2019

Asian J Pharm Clin Res

0

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Objective: The aim of the present study was the enhancement in the solubility of tamoxifen citrate using solid dispersion which is considered as a great solution to overcome the poor water solubility behavior of tamoxifen citrate (TMX) by solvent evaporation technique using Soluplus® as a novel carrier then formulate it as an orodispersible tablet.Method: A total of 24 formulas were prepared as a solid dispersion by solvent evaporation method using Soluplus® as a polymeric solubilizer in the ratio of 1:1, 1:3, 1:5, 1:7, and 1:10 then formulated as orodispersible tablets by incorporating three types of superdisintegrants; croscarmellose, crospovidone, and sodium starch glycolate (SSG) with the solid dispersion. Characterization of the formulation was done using differential scanning colorimetry, Fourier transforms infrared spectroscopy, X-ray diffraction, and scanning electron microscope and the best formula was selected according to the disintegration and dissolution tests.Results and Discussion: Formula 22 were selected as the best formula which contains mixed types of superdisintegrants; croscarmellose and SSG with the fastest complete disintegration of 6.5 s and complete dissolution with <2 min.Conclusion: Accordingly, TMX was successfully enhanced its water solubility by converting its crystalline structure into the amorphous state through solid dispersion with Soluplus® and formulated as an orodispersible tablet to improve its oral absorption.

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Lipid nanocarriers for tamoxifen citrate/coenzyme Q10 dual delivery

Cited by 24 publications

References 47 publications

Polymeric versus lipid nanocapsules for miconazole nitrate enhanced topical delivery: in vitro and ex vivo evaluation

Polymeric versus lipid nanocapsules for miconazole nitrate enhanced topical delivery: in vitro and ex vivo evaluation

Enhancement of the Solubility and the Dissolution Rate of Tamoxifen Citrate Solid Dispersion Using Soluplus by Solvent Evaporation Technique

Enhancement of the Solubility and the Dissolution Rate of Tamoxifen Citrate Solid Dispersion Using Soluplus by Solvent Evaporation Technique

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