Development, Characterization, and In Vitro Evaluation of Tamoxifen Microemulsions

Monteagudo, Ezequiel; Gándola, Yamila B.; González, Lorena; Bregni, Carlos; Carlucci, Adriana

doi:10.1155/2012/236713

Cited by 26 publications

(19 citation statements)

References 40 publications

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“…The electrical conductivity coefficient of T-ME and T-BSA-ME was revealed in 1.47 ms/cm and 2.49 ms/cm, respectively. the high value of conductivity coefficient is characteristic of oil-in-water (O/W) type of MEs (Table 3) [38, 39]. As can be seen, the conductivity coefficient of T-ME was higher than that of T-BSA-ME which was related to the higher percentage of water in T-ME compared with that of T-BSA-ME.…”

Section: Resultsmentioning

confidence: 99%

In vivo and in vitro biocompatibility study of novel microemulsion hybridized with bovine serum albumin as nanocarrier for drug delivery

Gharbavi

Manjili

Amani

et al. 2019

Heliyon

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The present study aimed to synthesize triacetin-microemulsion (T-ME) and T-ME hybridized with bovine serum albumin nanoparticles (T-BSA-ME) having narrow particle size distribution and versatile carrier systems as a novel microemulsion system. The suggested ME system was characterized by Fourier Transform Infrared spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Atomic Force Microscopy (AFM). The physicochemical properties of microemulsion system including particle size, PDI and ζ-potential, refractive index, Conductivity, %Transmittance, pH, and rheological behavior were also evaluated. In vivo biocompatibility was done using Median Lethal Dose (LD 50) calculated and trialed to evaluate the acute toxicity. In Addition, hemolysis and leukocyte proliferation assay were characterized to evaluate in-vitro biocompatibility of the suggested MEs systems. Moreover, cytotoxicity of MEs systems was also investigated on HFF-2 and HEK-293 cells. The presence of BSA NPs as a macromolecular biomaterial hybridized with T-ME reduced the cytotoxicity. The properties of the suggested MEs system proposed the T-ME hybridized with BSA-NPs as a promising candidate for co-delivery and multifunctional biomedicine applications.

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Section: Resultsmentioning

confidence: 99%

In vivo and in vitro biocompatibility study of novel microemulsion hybridized with bovine serum albumin as nanocarrier for drug delivery

Gharbavi

Manjili

Amani

et al. 2019

Heliyon

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“…62 Apart from improving drug dissolution, drug-loaded nanoparticles also have other biological activity, including sustained release and targeting of specific tissues and organs. Nanostructured lipid carriers have other advantages, including flexibility in route of administration, which may be either oral, parenteral, ocular, dermal, or pulmonary.…”

Section: Cytotoxic Effect Of Zer-nlc On a Leukemic Cell Linementioning

confidence: 99%

Zerumbone-loaded nanostructured lipid carriers: preparation, characterization, and antileukemic effect

Rahman¹,

Abdullah²,

How³

et al. 2013

IJN

134

121

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Zerumbone, a natural dietary lipophilic compound with low water solubility (1.296 mg/L at 25°C) was used in this investigation. The zerumbone was loaded into nanostructured lipid carriers using a hot, high-pressure homogenization technique. The physicochemical properties of the zerumbone-loaded nanostructured lipid carriers (ZER-NLC) were determined. The ZER-NLC particles had an average size of 52.68 ± 0.1 nm and a polydispersity index of 0.29 ± 0.004 µm. Transmission electron microscopy showed that the particles were spherical in shape. The zeta potential of the ZER-NLC was −25.03 ± 1.24 mV, entrapment efficiency was 99.03%, and drug loading was 7.92%. In vitro drug release of zerumbone from ZER-NLC was 46.7%, and for a pure zerumbone dispersion was 90.5% over 48 hours, following a zero equation. Using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay in human T-cell acute lymphoblastic leukemia (Jurkat) cells, the half maximal inhibitory concentration (IC 50 ) of ZER-NLC was 5.64 ± 0.38 µg/mL, and for free zerumbone was 5.39 ± 0.43 µg/mL after 72 hours of treatment. This study strongly suggests that ZER-NLC have potential as a sustainedrelease drug carrier system for the treatment of leukemia.

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“…Tamoxifen citrate (TMC) is BCS class II drug commercially converted to salt form as citrate to increase so as to increase its aqueous solubility and efficacy. Although it is in the salt form its solubility in water is limited as it has a higher melting point (146 ᵒC) which inhibits its dissolution [1].…”

Section: Introductionmentioning

confidence: 99%

Development of Tamoxifen Citrate Pellets by Hot-Melt Extrusion for Immediate Release: Study of Effect of Variables

Yadav

Kumar

2019

Int J App Pharm

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Objective: Objective of the study was to develop tamoxifen citrate immediate release pellets by hot-melt extrusion (HME) and to study the effect of various formulation and process variables. Methods: Pellets were prepared by HME technique. Effect of various parameters such as the concentration of ethylcellulose, PEG 6000, croscarmellose sodium, and spheronization speed were studied by using Central Composite Design. Pellets were evaluated for theoretical yield (%), mean pellet size (mm), sphericity (pellips), friability (%), porosity (%), mechanical crushing force (n), and dissolution efficiency. Optimized formulation was studied for compatibility study using IR, DSC, and XRD, SEM, In vitro drug release. In vitro Cell Cytotoxicity and Viability Assay were carried out using MCF-7 (human breast cancer cells) by MTT assay. Results: Results showed that a variable such as the amount of Methyl Cellulose, PEG 6000 and Spheronization speed showed positive correlation and amount of Croscarmellose sodium showed a negative correlation with dependent variables. Optimized formulation showed Korsmeyer Peppas model as a mechanism of drug release. Value of n was found to be in between 0.77+0.04, which reveals that, release mechanism of the drug as non-Fickian transport (0.45<n<0.89). MTT results of MCF-7 cells showed that optimized immediate release pellets have maximum cytotoxicity at 80 µg/ml. Conclusion: Study concluded that HME method and materials i.e. PEG 6000 and methylcellulose can effectively use to get immediate release of tamoxifen citrate so as to increase dissolution rate and cytotoxic effect.

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Development, Characterization, and In Vitro Evaluation of Tamoxifen Microemulsions

Cited by 26 publications

References 40 publications

In vivo and in vitro biocompatibility study of novel microemulsion hybridized with bovine serum albumin as nanocarrier for drug delivery

In vivo and in vitro biocompatibility study of novel microemulsion hybridized with bovine serum albumin as nanocarrier for drug delivery

Zerumbone-loaded nanostructured lipid carriers: preparation, characterization, and antileukemic effect

Development of Tamoxifen Citrate Pellets by Hot-Melt Extrusion for Immediate Release: Study of Effect of Variables

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