“…Therefore, 0.5% w/v P407 concentration was selected as the optimum concentration for additional investigations. Our results were in good agreement with Freag et al 47 who reported that 0.5% w/v P407 concentration relative to total dispersion volume was quite sufficient to stabilize LCNPs and maintain their internal structure.…”
Section: Effect Of Stabilizer Concentrationsupporting
confidence: 93%
“…The concentration of hydrotropes represented 70% w/w of the amount of GMO. 47 As summarized in Table 1, ethanol (F3) possessed a great tendency in reducing the viscosity of GMO which in turn facilitates prompt diffusion of the hydrotropic mixture into aqueous phase. This was evidenced by significant (P,0.05) decrease in both PS and PDI compared to (F1, propylene glycol; F2, PEG 400).…”
Section: Preparation Of Ion-paired Pmx-rsv-lcnpsmentioning
BackgroundLung cancer is the most common cancer and the leading cause of total deaths worldwide. Its classified into two major types including non-small cell lung carcinoma (NSCLC) and small cell lung carcinoma (SCLC) based on the origin of abnormal lung cells as well as the smoking status of the patient. NSCLC is the most common and aggressive type of lung cancer representing 80%–85% of all cases.PurposeThe aim of the study was to present lyotropic liquid crystalline nanoparticles (LCNPs) as promising carriers for co-delivery of the chemotherapeutic agent, pemetrexed (PMX) and the herbal drug, resveratrol (RSV) for effective lung cancer management.MethodsThe proposed PMX-RSV-LCNPs were prepared by hydrotrope method. Hydrophobic ion pairing with cetyl trimethyl ammonium bromide (CTAB) was implemented to increase the encapsulation efficiency of the hydrophilic PMX up to 95%±3.01%.ResultsThe tailored PMX-RSV-LCNPs exhibited a particle size of 173±0.26 nm and biphasic release pattern with a relatively initial burst release within first 3–4 hour followed by sustained release up to 24 hours. Moreover, PMX-RSV-LCNPs manifested superior concentration and time dependent cytotoxicity profile against A549 lung cancer cells with IC50 4.0628 µg/mL. Besides, the enhanced cellular uptake profile based on bioadhesive properties of glyceryl monoolein (GMO) as well as energy independent (cholesterol dependent) pattern. In-vivo evaluations against urethane induced lung cancer bearing mice demonstrated the potentiality of PMX-RSV-LCNPs in tumor growth inhibition via inhibition of angiogenesis and induction of apoptosis. The results were supported by histopathological analysis and immunohistochemical Ki67 staining. Moreover, PMX-RSV-LCNPs displayed a promising safety profile via attenuating nephro- and hepatotoxicity.ConclusionPMX-RSV-LCNPs elaborated in the current study hold a great promise for lung cancer treatment.
“…Therefore, 0.5% w/v P407 concentration was selected as the optimum concentration for additional investigations. Our results were in good agreement with Freag et al 47 who reported that 0.5% w/v P407 concentration relative to total dispersion volume was quite sufficient to stabilize LCNPs and maintain their internal structure.…”
Section: Effect Of Stabilizer Concentrationsupporting
confidence: 93%
“…The concentration of hydrotropes represented 70% w/w of the amount of GMO. 47 As summarized in Table 1, ethanol (F3) possessed a great tendency in reducing the viscosity of GMO which in turn facilitates prompt diffusion of the hydrotropic mixture into aqueous phase. This was evidenced by significant (P,0.05) decrease in both PS and PDI compared to (F1, propylene glycol; F2, PEG 400).…”
Section: Preparation Of Ion-paired Pmx-rsv-lcnpsmentioning
BackgroundLung cancer is the most common cancer and the leading cause of total deaths worldwide. Its classified into two major types including non-small cell lung carcinoma (NSCLC) and small cell lung carcinoma (SCLC) based on the origin of abnormal lung cells as well as the smoking status of the patient. NSCLC is the most common and aggressive type of lung cancer representing 80%–85% of all cases.PurposeThe aim of the study was to present lyotropic liquid crystalline nanoparticles (LCNPs) as promising carriers for co-delivery of the chemotherapeutic agent, pemetrexed (PMX) and the herbal drug, resveratrol (RSV) for effective lung cancer management.MethodsThe proposed PMX-RSV-LCNPs were prepared by hydrotrope method. Hydrophobic ion pairing with cetyl trimethyl ammonium bromide (CTAB) was implemented to increase the encapsulation efficiency of the hydrophilic PMX up to 95%±3.01%.ResultsThe tailored PMX-RSV-LCNPs exhibited a particle size of 173±0.26 nm and biphasic release pattern with a relatively initial burst release within first 3–4 hour followed by sustained release up to 24 hours. Moreover, PMX-RSV-LCNPs manifested superior concentration and time dependent cytotoxicity profile against A549 lung cancer cells with IC50 4.0628 µg/mL. Besides, the enhanced cellular uptake profile based on bioadhesive properties of glyceryl monoolein (GMO) as well as energy independent (cholesterol dependent) pattern. In-vivo evaluations against urethane induced lung cancer bearing mice demonstrated the potentiality of PMX-RSV-LCNPs in tumor growth inhibition via inhibition of angiogenesis and induction of apoptosis. The results were supported by histopathological analysis and immunohistochemical Ki67 staining. Moreover, PMX-RSV-LCNPs displayed a promising safety profile via attenuating nephro- and hepatotoxicity.ConclusionPMX-RSV-LCNPs elaborated in the current study hold a great promise for lung cancer treatment.
“…Moreover, the targeted and non-targeted NPs (F3 and F2, respectively) also succeeded to significantly (p < 0.05) reduce the level of angiogenic factor VEGF-1 by 5.125- and 2.883-folds, respectively versus 2.127-folds reduction for free RSV/PMT combination as compared to the positive control (Fig. 11a) [28]. Fig.…”
Section: Resultsmentioning
confidence: 99%
“…Tumor growth was estimated daily until its volume reached 100 mm 3 . Tumor volume was determined by measuring both perpendicular diameters of the tumor using a micrometer based on the following equation [28]:where W is tumor width, L is tumor length.…”
BackgroundThe rationale of this study is to combine the merits of both albumin nanoparticles and quantum dots (QDs) in improved drug tumor accumulation and strong fluorescence imaging capability into one carrier. However, premature drug release from protein nanoparticles and high toxicity of QDs due to heavy metal leakage are among challenging hurdles. Following this platform, we developed cancer nano-theranostics by coupling biocompatible albumin backbone to CdTe QDs and mannose moieties to enhance tumor targeting and reduce QDs toxicity. The chemotherapeutic water soluble drug pemetrexed (PMT) was conjugated via tumor-cleavable bond to the albumin backbone for tumor site-specific release. In combination, the herbal hydrophobic drug resveratrol (RSV) was preformulated as phospholipid complex which enabled its physical encapsulation into albumin nanoparticles.ResultsAlbumin–QDs theranostics showed enhanced cytotoxicity and internalization into breast cancer cells that could be traced by virtue of their high fluorescence quantum yield and excellent imaging capacity. In vivo, the nanocarriers demonstrated superior anti-tumor effects including reduced tumor volume, increased apoptosis, and inhibited angiogenesis in addition to non-immunogenic response. Moreover, in vivo bioimaging test demonstrated excellent tumor-specific accumulation of targeted nanocarriers via QDs-mediated fluorescence.ConclusionMannose-grafted strategy and QD-fluorescence capability were beneficial to deliver albumin nanocarriers to tumor tissues and then to release the anticancer drugs for killing cancer cells as well as enabling tumor imaging facility. Overall, we believe albumin–QDs nanoplatform could be a potential nano-theranostic for bioimaging and targeted breast cancer therapy.Electronic supplementary materialThe online version of this article (10.1186/s12951-019-0445-7) contains supplementary material, which is available to authorized users.
“…Moreover, the targeted nanoparticles also enhanced in vivo tumor growth inhibition rate in Ehrlich ascites tumor-bearing mice. 29 For traditional/herbal medicines, HA has also been used for conjugation on the surface of nanoparticles delivering 3,4-difluorobenzylidene curcumin resulting in increased cellular uptake and cytotoxic activity of the drug against human pancreatic cancer cells (MiaPaCa-2 and AsPC-1) compared with non-targeted nanoparticles (mean IC 50 : 140 nM, 160 nM, and 245 nM, respectively). Interestingly, when the CD44 receptor was blocked by free soluble HA, the cytotoxic activity to MiaPaCa-2 cells was comparable between the targeted and non-targeted nanoparticles (mean IC 50 : 234 nM and 245 nM, respectively).…”
Patients treated with conventional cancer chemotherapy suffer from side effects of the drugs due to non-selective action of chemotherapeutic drugs to normal cells. Active targeting nanoparticles that are conjugated to targeting ligands on the surface of nanoparticles play an important role in improving drug selectivity to the cancer cell. Several chemotherapeutic drugs and traditional/herbal medicines reported for anticancer activities have been investigated for their selective delivery to cancer cells by active targeting nanoparticles. This systematic review summarizes reports on this application. Literature search was conducted through PubMed database search up to March 2017 using the terms nanoparticle, chemotherapy, traditional medicine, herbal medicine, natural medicine, natural compound, cancer treatment, and active targeting. Out of 695 published articles, 61 articles were included in the analysis based on the predefined inclusion and exclusion criteria. The targeting ligands included proteins/peptides, hyaluronic acid, folic acid, antibodies/antibody fragments, aptamer, and carbohydrates/polysaccharides. In vitro and in vivo studies suggest that active targeting nanoparticles increase selectivity in cellular uptake and/or cytotoxicity over the conventional chemotherapeutic drugs and non-targeted nanoparticle platform, particularly enhancement of drug efficacy and safety. However, clinical studies are required to confirm these findings.
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