Development of tamoxifen‐loaded surface‐modified nanostructured lipid carrier using experimental design:
            <i>in vitro</i>
            and
            <i>ex vivo</i>
            characterisation

Ganesan, P.; Damodharan, N

doi:10.1049/iet-nbt.2019.0276

Cited by 11 publications

(4 citation statements)

References 69 publications

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“…The protection was even more evident when NLCs were used. This was in concordance with the previous studies [55,56]) This may be related to the protection of the drug and the controlled release of LC [57]. Moreover, this decreased toxicity allows chronic use of LC molecules with decreased side effects.…”

Section: Cell Viability and Toxicology Studysupporting

confidence: 92%

Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity

Uner,

Ergin,

Ansari

et al. 2023

Molecules

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Addressing obesity is a critical health concern of the century, necessitating urgent attention. L-carnitine (LC), an essential water-soluble compound, plays a pivotal role in lipid breakdown via β-oxidation and facilitates the transport of long-chain fatty acids across mitochondrial membranes. However, LC’s high hydrophilicity poses challenges to its diffusion through bilayers, resulting in limited bioavailability, a short half-life, and a lack of storage within the body, mandating frequent dosing. In our research, we developed LC-loaded nanoparticle lipid carriers (LC-NLCs) using economically viable and tissue-localized nanostructured lipid carriers (NLCs) to address these limitations. Employing the central composite design model, we optimized the formulation, employing the high-pressure homogenization (HPH) method and incorporating Poloxamer® 407 (surfactant), Compritol® 888 ATO (solid lipid), and oleic acid (liquid oil). A comprehensive assessment of nanoparticle physical attributes was performed, and an open-field test (OFT) was conducted on rats. We employed immunofluorescence assays targeting CRP and PPAR-γ, along with an in vivo rat study utilizing an isolated fat cell line to assess adipogenesis. The optimal formulation, with an average size of 76.4 ± 3.4 nm, was selected due to its significant efficacy in activating the PPAR-γ pathway. Our findings from the OFT revealed noteworthy impacts of LC-NLC formulations (0.1 mg/mL and 0.2 mg/mL) on adipocyte cells, surpassing regular L-carnitine formulations’ effects (0.1 mg/mL and 0.2 mg/mL) by 169.26% and 156.63%, respectively (p < 0.05).

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Section: Cell Viability and Toxicology Studysupporting

confidence: 92%

Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity

Uner,

Ergin,

Ansari

et al. 2023

Molecules

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“…The same profile was observed in the absence of serum supplementation, in which BEAS-2B cells were also more susceptible than A549 cells for NLC-RSO treatment (25 μg/mL) (data not shown). Therefore, the effective delivery of NLC containing the bioactive oil was observed after 24 h when compared to the NLC without bioactives and this process can lead to a reduction in the cellular toxicity ( Poovi and Damodharan, 2020 ; Moura et al, 2021 ).…”

Section: Resultsmentioning

confidence: 99%

Red sacaca essential oil-loaded nanostructured lipid carriers optimized by factorial design: cytotoxicity and cellular reactive oxygen species levels

Chura,

Memória,

Lopes

et al. 2023

Front. Pharmacol.

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Amazonian flora includes several species with the potential to develop pharmaceutical and biotechnological products. The essential oils from Amazonian species possess some biological properties, such as antioxidant, antibacterial, and cytotoxic activities. The essential oil of red sacaca (RSO), Croton cajucara Benth., contains metabolites characterized by antioxidant and anti-inflammatory activities. Nanostructured lipid carriers (NLC) are an advantageous alternative for the effective delivery of drugs because they can solubilize lipophilic actives and reduce their cytotoxicity. This study aimed to optimize the synthesis of RSO-loaded nanostructured lipid carriers (NLC-RSO) using a 23 factorial design and investigate their antioxidant and cytotoxic effects. The red sacaca essential oil (RSO) metabolite profile was characterized using gas chromatography coupled with a mass spectrometer (GC-MS), identifying 33 metabolites, with linalool and 7-hydroxy-calamenene as the major ones, as reported in the literature. The optimized NLC-RSO formulation had a particle size less than 100 nm and a polydispersity index lower than 0.25. After characterizing NLC-RSO using Fourier-transform infrared spectroscopy, powder X-ray diffraction, zeta potential, moisture content, and wettability, in vitro cytotoxicity were performed in A549 and BEAS-2B cell lines using the resazurin metabolism assay. The data indicated a lower IC50 for RSO than for NLC-RSOs in both cell lines. Furthermore, low cytotoxicity of blank nanoparticles (blank NP) and medium chain triglycerides-loaded nanostructured lipid carriers (NLC-MCT) towards both pulmonary cell lines was noted. At a concentration of 50–100 μg/mL, free RSO exhibited higher cytotoxicity than NLC-RSO, demonstrating the protective effect of this lipid carrier in reducing cytotoxicity during metabolite delivery. Similarly, free RSO showed higher 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging than NLC-RSO, also indicating this protective effect. The 2′,7′-dichlorofluorescein diacetate (DCFH-DA) intracellular reactive oxygen species (ROS) level assay did not show differences between the treatments at higher but non-cytotoxic dosages. Taken together, our results suggest that NLC-RSOs are potential RSO delivery systems for applications related to cancer treatment.

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“…Efek tersebut diketahui dengan mengukur penanda aktivitas sel, seperti aktivitas metabolisme, jumlah sel yang ada atau pembelahan yang terjadi, produksi ATP atau pun sintesis DNA (11). Pada penelitian Poovi & Damodharan (20), cell viability assay dilakukan pada sel MCF-7, yang merupakan galur sel kanker payudara. % cell viability tamoxifen sebelum dan setelah dibuat dalam sistem NLC masing-masing adalah 70% dan 50%.…”

Section: Metode Pembuatan Sistem Nanocarrier Berbasis Lipidunclassified

Kajian Pengembangan Sistem Nanocarrier Berbasis Lipid untuk Penghantaran Tamoxifen pada Terapi Endokrin Kanker Payudara

Elisa,

Aryani,

Mulyanti

2023

BCSP

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Abstract. Tamoxifen is an antiestrogen that is the first line of endocrine therapy for breast cancer with HR+. The active substance has very low water solubility (about 0.3 mg/L) and metabolism in the liver, resulting in low bioavailability. Various lipid-based drug delivery systems can be developed to increase the effectiveness and reduce the side effects of tamoxifen. This study aims to determine the strategy for developing lipid-based nanocarrier systems in the form of liposomes, niosomes, SLNs, and NLCs in the delivery of tamoxifen, as well as to find the best nanocarrier system to increase the effectiveness and reduce the side effects of tamoxifen. This study was conducted using the Systematic Literature Review (SLR) method. The results showed that tamoxifen formulated in NLC form, with GMS as solid lipid components, olive oil as liquid lipids, POE-40-S as surfactant, PVA as co-surfactant, and prepared by microemulsion-cooling method provided the best characteristics of lipid-based nanocarrier systems, and stable. Liposome and NLC systems showed the greatest increase in the effectiveness of tamoxifen, marked by increased growth inhibition of MCF-7, MDA MB-231 cells, pharmacokinetic data (Cmax and AUC), and survival of the test animals. In addition, the development of lipid nanocarriers can also reduce the hepatotoxicity of tamoxifen, such as reducing ALT and AST levels. Keywords: Tamoxifen, Nanocarrier, Lipids. Abstrak. Tamoxifen merupakan antiestrogen yang menjadi first line untuk terapi endokrin kanker payudara dengan HR+. Zat aktif tersebut memiliki kelarutan dalam air yang sangat rendah (sekitar 0,3 mg/L) dan mengalami metabolisme di hati, sehingga bioavailabilitasnya rendah. Berbagai sistem penghantaran obat berbasis lipid dapat dikembangkan untuk mencapai peningkatan efektifitas dan penurunan efek samping tamoxifen. Kajian ini bertujuan untuk mengetahui strategi pengembangan sistem nanocarrier berbasis lipid dalam bentuk liposom, niosom, SLN, dan NLC dalam penghantaran tamoxifen, serta mendapatkan sistem nanocarrier yang paling baik untuk meningkatkan efektifitas dan menurunkan efek samping tamoxifen. Kajian ini dilakukan dengan metode Systematic Literature Review (SLR). Hasil kajian menunjukkan bahwa tamoxifen yang diformulasikan dalam bentuk NLC, dengan komponen lipid padat GMS, lipid cair minyak zaitun, surfaktan POE-40-S dan ko-surfaktan PVA, serta dibuat dengan metode mikroemulsi-pendinginan memberikan karakteristik sistem nanocarrier berbasis lipid yang paling baik dan stabil. Sistem liposom dan NLC menunjukkan peningkatan efektifitas tamoxifen yang paling besar ditandai dengan meningkatnya penghambatan pertumbuhan sel MCF-7, MDA MB-231, data farmakokinetik (Cmax dan AUC), serta kelangsungan hidup hewan uji. Selain itu, pengembangan lipid nanocarrier juga dapat mengurangi hepatotoksik tamoxifen, seperti menurunkan kadar ALT dan AST. Kata Kunci: Tamoxifen, Nanocarrier, Lipid.

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Development of tamoxifen‐loaded surface‐modified nanostructured lipid carrier using experimental design: in vitro and ex vivo characterisation

Cited by 11 publications

References 69 publications

Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity

Assessing the In Vitro and In Vivo Performance of L-Carnitine-Loaded Nanoparticles in Combating Obesity

Red sacaca essential oil-loaded nanostructured lipid carriers optimized by factorial design: cytotoxicity and cellular reactive oxygen species levels

Kajian Pengembangan Sistem Nanocarrier Berbasis Lipid untuk Penghantaran Tamoxifen pada Terapi Endokrin Kanker Payudara

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