Enhancing the Therapeutic Efficacy of Tamoxifen Citrate Loaded Span-Based Nano-Vesicles on Human Breast Adenocarcinoma Cells

Kassem, Mohammed A.; Megahed, Mohamed A.; Elyazid, Sherif K. Abu; Abd-Allah, Fathy I.; Abdelghany, Tamer M.; Al‐Abd, Ahmed M.; El-Say, Khalid M.

doi:10.1208/s12249-018-0962-y

Cited by 21 publications

(15 citation statements)

References 87 publications

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“…Besides, it might be due to the electrostatic attractions between the cationic drug and the negatively charged vesicles. Similar observations were obtained in tamoxifen citrate loaded span-based nanovesicles [20].…”

Section: Entrapment Efficiency (Ee %)supporting

confidence: 85%

Benazepril Hydrochloride Loaded Niosomal Formulation for Oral Delivery: Formulation and Characterization

Radhi

2018

Int J App Pharm

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Objective: The objective of the present study was to formulate niosomal formulations of benazepril hydrochloride in an attempt to overcome the hurdles associated with itʼs poor oral absorption.Methods: Nine formulations were prepared with various ratios of sorbitan monostearate (span 60), sorbitan monopalmitate (span 40) and polyoxyethylene 2 stearyl ether (brij 72) as non-ionic surfactants, cholesterol as a stabilizing agent and soya lecithin as a charge imparting agent. Then, they were characterized for vesicle size, polydispersity (PDI), entrapment efficiency (EE %), release profile, zeta (ζ) potential and transmission electron microscopy (TEM).Results: Niosomal formulations exhibited an efficient entrapment range between (80.4-97.8) percent, vesicles size analyses revealed the formation of homogenously dispersed vesicles having a size range of (3.9±1.7-8.72±4.4) micrometers. The in vitro release studies revealed that all formulations displayed sustained release in comparison with the pure drug. Formulations prepared with span 60 and span 40 possessed adequate stability according to zeta potential analysis, whereas brij 72 failed the test and possessed inadequate zeta potential range. TEM images of the optimized formulations (F7 and F8) have confirmed the formation of vesicles with spherical shapes.Conclusion: Based on the study results, niosomal formulations seem to be attractive alternatives to conventional delivery for benazepril hydrochloride.

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Section: Entrapment Efficiency (Ee %)supporting

confidence: 85%

Benazepril Hydrochloride Loaded Niosomal Formulation for Oral Delivery: Formulation and Characterization

Radhi

2018

Int J App Pharm

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“…According to the World Health Organization estimates, by 2030, the global incidence is expected to increase to 21.7 million cancer cases [1][2][3]. Currently, chemotherapy is one of the most effective strategies to avoid the proliferation of malignant tumors [3,4]. However, the ability of cancer cells to become resistant to different drugs remains a significant impediment to successful chemotherapy [1].…”

Section: Introductionmentioning

confidence: 99%

Repositioning of Anti-parasitic Drugs in Cyclodextrin Inclusion Complexes for Treatment of Triple-Negative Breast Cancer

Priotti

Baglioni²,

Garcı́a

et al. 2018

AAPS PharmSciTech

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This e-offprint is for personal use only and shall not be self-archived in electronic repositories. If you wish to self-archive your article, please use the accepted manuscript version for posting on your own website. You may further deposit the accepted manuscript version in any repository, provided it is only made publicly available 12 months after official publication or later and provided acknowledgement is given to the original source of publication and a link is inserted to the published article on Springer's website. The link must be accompanied by the following text: "The final publication is available at link.springer.com". Abstract.Drug repositioning refers to the identification of new therapeutic indications for drugs already approved. Albendazole and ricobendazole have been used as anti-parasitic drugs for many years; their therapeutic action is based on the inhibition of microtubule formation. Therefore, the study of their properties as antitumor compounds and the design of an appropriate formulation for cancer therapy is an interesting issue to investigate. The selected compounds are poorly soluble in water, and consequently, they have low and erratic bioavailability. In order to improve their biopharmaceutics properties, several formulations employing cyclodextrin inclusion complexes were developed. To carefully evaluate the in vitro and in vivo antitumor activity of these drugs and their complexes, several studies were performed on a breast cancer cell line (4T1) and BALB/c mice. In vitro studies showed that albendazole presented improved antitumor activity compared with ricobendazole. Furthermore, albendazole:citrate-β-cyclodextrin complex decreased significantly 4T1 cell growth both in in vitro and in vivo experiments. Thus, new formulations for anti-parasitic drugs could help to reposition them for new therapeutic indications, offering safer and more effective treatments by using a well-known drug.

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“…Finally at an equal level of X 1 , X 2 and X 4 , increasing the DCP amount from 6.59 mg to 23.4 mg will increase EE% from 68.3% to 79.5% for F18 and F5 respectively, also increasing the DCP amount from 10 mg to 20 mg will increase EE% from 86.9% to 87.8% for F7 and F15 respectively. The attraction forces between negatively charged DCP and the positively charged drug may be a good explanation of this finding [37]. The mathematical equation that best fits the model is:…”

Section: Estimation Of the Quantitative Effects Of The Factors Effects On The Mean Particle Size (Y 1 )mentioning

confidence: 96%

“…Based on the literature, the two main factors affecting niosomal formulation are cholesterol and nonionic surfactants in addition to DCP as a negative surface charge-inducer to lower the probability of aggregation and increase formulation stability. [37]. A threelevel four-factor D-LSCD design was used for statistical optimization of the formulation variables for preparing FLT-loaded niosomes.…”

Section: Experimental Designmentioning

confidence: 99%

Cholesterol-Based Nanovesicles Enhance the In Vitro Cytotoxicity, Ex Vivo Intestinal Absorption, and In Vivo Bioavailability of Flutamide

et al. 2021

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Critical adverse effects and frequent administration, three times per day, limit the use of flutamide (FLT) as a chemotherapeutic agent in the treatment of prostate cancer. Therefore, our research aimed to develop new cholesterol-based nanovesicles for delivering FLT to malignant cells in an endeavor to maximize its therapeutic efficacy and minimize undesired adverse effects. Draper–Lin small composite design was used to optimize the critical quality attributes of FLT-loaded niosomes and ensure the desired product quality. The influence of the selected four independent variables on mean particle size (Y1), zeta potential (Y2), drug entrapment efficiency (Y3), and the cumulative drug release after 24 h (Y4) was examined. The optimized nanovesicles were assessed for their in vitro cytotoxicity, ex-vivo absorption via freshly excised rabbit intestine as well as in vivo pharmacokinetics on male rats. TEM confirmed nanovescicles’ spherical shape with bilayer structure. Values of dependent variables were 748.6 nm, −48.60 mV, 72.8% and 72.2% for Y1, Y2, Y3 and Y4, respectively. The optimized FLT-loaded niosomes exerted high cytotoxic efficacy against human prostate cancer cell line (PC-3) with an IC50 value of 0.64 ± 0.04 µg/mL whilst, it was 1.88 ± 0.16 µg/mL for free FLT. Moreover, the IC50 values on breast cancer cell line (MCF-7) were 0.27 ± 0.07 µg/mL and 4.07 ± 0.74 µg/mL for FLT-loaded niosomes and free FLT, respectively. The permeation of the optimized FLT-loaded niosomes through the rabbit intestine showed an enhancement ratio of about 1.5 times that of the free FLT suspension. In vivo pharmacokinetic study displayed an improvement in oral bioavailability of the optimized niosomal formulation with AUC and Cmax values of 741.583 ± 33.557 μg/mL × min and 6.950 ± 0.45 μg/mL compared to 364.536 ± 45.215 μg/mL × min and 2.650 ± 0.55 μg/mL for the oral FLT suspension. With these promising findings, we conclude that encapsulation of FLT in cholesterol-loaded nanovesicles enhanced its anticancer activity and oral bioavailability which endorse its use in the management of prostate cancer.

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Enhancing the Therapeutic Efficacy of Tamoxifen Citrate Loaded Span-Based Nano-Vesicles on Human Breast Adenocarcinoma Cells

Cited by 21 publications

References 87 publications

Benazepril Hydrochloride Loaded Niosomal Formulation for Oral Delivery: Formulation and Characterization

Benazepril Hydrochloride Loaded Niosomal Formulation for Oral Delivery: Formulation and Characterization

Repositioning of Anti-parasitic Drugs in Cyclodextrin Inclusion Complexes for Treatment of Triple-Negative Breast Cancer

Cholesterol-Based Nanovesicles Enhance the In Vitro Cytotoxicity, Ex Vivo Intestinal Absorption, and In Vivo Bioavailability of Flutamide

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