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. 2021 Dec 24;12:787226. doi: 10.3389/fphar.2021.787226

TABLE 2.

The summary of literature reviews for UA-loaded nanoparticles.

No Code Carrier type Formula-tion Type of research Information research Administra-tion route Reference
1 Lipo A Liposomes Not Available Phase I Clinical Trials Safety Evaluation of Double Dose and Antitumor Activity of Ursolic Acid (UAL) Liposomes in Subjects with Advanced Solid Tumors including: Non-Hodgkin Lymphoma (24%), Hodgkin Lymphoma (24%), Renal Carcinoma (5%), Hepatocellular Carcinoma (5%), Breast Cancer (9%), Lung Cancer (9%), Other Cancers (19%) Intravenous 4 h infusion at doses equivalent to 54, 74, and 96 mg UA/m2 for 14 consecutive days Qian et al. (2015)
2 Lipo B Liposomes Not Available Phase I Clinical Trials Toxicity evaluation of a single dose of intravenous ursolic acid liposomes (UAL) in healthy adult volunteers and patients with advanced solid tumors including Non-Hodgkin Lymphoma, Hodgkin Lymphoma, Renal Carcinoma, and Hepatocellular Carcinoma Intravenous (IV) route at doses equivalent to 11, 22, 37, 56, 74, and 96, and 130 mg UA/m2 administered as a 4 h infusion Wang et al. (2013)
3 Lipo C Liposomes Not Available Phase I Clinical Trials Toxicity evaluation of Ursolic Acid Nanoliposome (UANL) in healthy volunteers and patients with advanced solid tumors including: Non-Hodgkin Lymphoma (50%), Hodgkin Lymphoma (12.5%), Gut Cancer (12.5%), Hepatocellular Carcinoma (25%) Intravenous (IV) route at doses equivalent to 74 mg/m2 as a single dose, 98 mg/m2, and 74 mg/m2 as double doses daily for 14 days via a 4 h infusion Zhu et al. (2013)
4 Lipo D Liposomes Hydrophobic components (PC, Chl, and UA) at a weight ratio of 2:1:0.5; ethanol injection method Preclinical or in vivo study Tumor inhibition activity and toxicity studies of UA-PLL-HA in SCC-7 tumor-induced mice Intravenous (IV) at a dose of equivalent to 20 mg UA/Kg mouse for 5 times every 4 days Poudel et al. (2020)
5 Lipo E Liposomes PEGylated UA Liposomes composed of SPC, CHOL, and UA at a weight ratio of 50:8:5, respectively; ethanol injection method Preclinical or in vivo study Tumor growth inhibition study and cytotoxicity of UA PEGylated liposomes in mice with U14 cervical carcinoma cells Intragastric route at a dose of equivalent to 80 mg UA/kg mouse twice a day for a total of 14 days Wang et al. (2016)
6 Lipo F Liposomes Liposomes composed of hydrophobic components (SPC, CHOL and UA) at a weight ratio of 0:6:5; ethanol injection method Preclinical or in vivo study Tumor growth inhibition and toxicity studies of CS-UA-L in mice with U14 cervical carcinoma cells Intragastric route at a dose of equivalent to 80 mg UA/Kg mouse once a day for 14 days Wang et al. (2017)
7 Lipo G Liposomes Lipids-UA (HSPC/Kolesterol/DSPE-PEG2000/UA = 90/0/5/5 and 90/0/5/10, (molar ratio); thin film hydration method Preclinical or in vivo study Tumor and growth inhibition study of UA-L in mice with 4T1 tumors (breast cancer) Intravenous (IV) route at a dose of equivalent to 10 mg UA/kg mouse for 5 times every other day Zhang et al. (2020)
8 Lipo H Liposomes Lipid components of FA-UA-L: DOTAP/CHOL/MPEG-DSPE2000/FA-PEG-CHEMS at a molar ratio of 40:55:4, 5:0, 5 (equal to weight ratio of 28; 21,3; 12,6, dan 2, 1 mg). The ratio of UA to lipid is 1:20 (w/w); thin film hydration method Preclinical or in vivo study Tumor growth inhibition and toxicity studies of FA-UA/siRNA-L in mice with human kB cells tumor Intravenous (IV) injection with the dose of 4.5 mg/kg for UA and 170 μg/kg for siRNA for 5 times every other day Li et al. (2019)
9 Lipo I Liposomes Lipid composition: HSPC/CHOL/mPEG-DSPE2000/FA-PEG-CHEMS at molar ratio 63:32:4.5:0.5 (equal to weights amount of 48, 12, 13.4, and 5 mg), respectively. The ratio of UA to lipids is 1:20 (w/w); thin film hydration method Preclinical or in vivo study Efficacy study of FTL-UA for tumor inhbition in mice with human KB tumor cells Intravenous (IV) at a dose of equivalent to 4.5 mg UA/kg mouse for 5 times every other day, which is similar to 23 mg/kg or 98 mg/m2 drug administration Yang et al. (2014)
10 Nano A Nanospheres Not available Preclinical or in vivo study Tumor growth inhibition and toxicity studies of HCPT @F-Pt-PU NPs in mice with H22 subcutaneous tumors (liver cancer) Intravenous (IV) injection at a dose of equivalent to 10 mg UA/kg mouse for 5 times every 2 days Liu et al. (2021)
11 Nano B Nanospheres NP composed of 32 mg chitosan, 10 mg UA, 30 mg EDC, and 8 mg NHS. The ratio of UA to lipids is 1:10 (w/w); overnight magnetic stirring method Preclinical or in vivo study Tumor inhibition study of CH-UA-NPs in mice with H22 subcutaneous tumors (liver cancer) Oral administration at a dose of equivalent to 11 mg UA/Kg mouse once every 2 days for a total of 8 times Jin et al. (2016a)
12 Nano C Nanospheres NP composed of 32 mg chitosan, 10 mg UA, 30 mg EDC, and 8 mg NHS. The ratio of UA to lipids is 1:10 (w/w); overnight magnetic stirring method Preclinical or in vivo study FA-CS-UA-NPs tumor inhibiting activity study in MCF-7 xenograft bearing models (breast cancer) Intraperitoneal (IP) injection at a dose of equivalent to 12.5 mg UA/kg mouse once a day for 9 times Jin et al. (2016b)
13 Nano D Nanospheres Not available Preclinical or in vivo study Tumor growth inhibition efficacy and toxicity studies of UA-LA-ICG NPs in tumor bearing mice by murine H22-hepatocarcinoma cells induced tumor xenograft models Intravenous (IV) injection at a dose of 10 mg/kg of UA and 2.5 mg/kg of ICG with 5 min irradiation at 24 h post injection Zhao et al. (2018)
14 Nano E Nanospheres Prepared by making 3 mg UA solution in ethanol (1 ml, 6,569 mM) in 10 ml of water. The ratio of UA and NPs was 1:10, respectively; solvent exchange preparation method Preclinical or in vivo study Tumor inhibition efficacy and toxicity studies of UA NPs in mice bearing A549 xenograft models (lung cancer) Intravenous (IV) injection at a dose of 8 mg/kg of UA for 21 days Fan et al. (2018)
15 Nano F Nanospheres Not available Preclinical or in vivo study Tumor inhibiting activity and toxicity studies of UA NPs in H22-induced mice (Hepatocellular carcinoma) Intraperitoneal (IP) injection at a daily dose of 50 mg/kg of UA for 10 days Zhang et al. (2015)
16 Nano G Nanospheres Self-assembly method of polymer deposition Preclinical or in vivo study Antitumor activity and toxicity studies of Pec-8PUH NPs in mice with 4T1 tumors (breast cancer) Intravenous (IV) injection at a dose of 10 mg/kg of UA once every 2 days for 5 times Liu et al. (2018)
17 Poli A Polymeric Micelles PM composed of UA (4 mg) and mPEG2000-PLA2000 (40 mg) at a weight ratio of 1:10; thin film dispersion method Preclinical or in vivo study Antitumor activity and toxicity studies of UA-PMs in H22-induced mice (Hepatocellular carcinoma) Intraperitoneal (IP) injection at a dose of 50 mg/kg of UA every 2 days for 6 times Zhou et al. (2019)
18 Poli B Polymeric Micelles Solvent evaporation method Preclinical or in vivo study Antitumor activity and toxicity studies of U-SS-M in tumor bearing MG-63/Osteosarcoma (OS) Intravenous (IV) injection at a dose of 11 mg/kg of UA every 3 days for 5 times Fu et al. (2021)

Notes: UAL, Ursolic Acid Liposome; UANL, Ursolic Acid Nanoliposome; UA-PLL-HA, Ursolic Acid-Poly-L-Lysine-Hyaluronic Acid; UA-PEGylated, Ursolic Acid-Polietilenglikolisasi; CH-UA-NPs, Chitosan-Ursolic Acid-Nanoparticles; CS-UA-L, Chitosan- Ursolic Acid-Liposome; CHOL/Chl, Cholesterol; DSPE-PEG2000, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N [methoxy (poly- ethylene glycol) -2000]; DOTAP, 1, 2-dioleoyl-3-trimethylammonium-propane; EDC, Ethyl-(3-3-dimethylaminopropyl) carbondiimide hydrochloride; FA-CS-UA-NPs, Folate- Chitosan-Ursolic Acid-Nanoparticles; FA-PEG-CHEMS, Folate Polyethylene Glycol Cholesteryl hemisuccinate; FA-UA/siRNA-L, Folate- Ursolic Acid/Small Interfering RNA-Liposome; F-Pt-PU, Folic Acid-Pectin-Eight-Arm PEG-UA conjugate; FTL-UA, Folate Receptor Targeted Liposome-Ursolic Acid; HCPT @F-Pt-PU NPs, Hydroxycamptothecin @folic acid-pectin-eight-arm PEG-UA nanoparticle; HSPC, Hydrogenated Soybean Phosphatidyl Choline; mPEG2000-PLA2000, Monomethoxy Polyethylene Glycol 2000 Poly Lactic Acid 2000; MPEG-DSPE2000, Monomethoxy Polyethylene Glycol 2000-Distearoyl Phosphatidylethanolamine; NHS, N-Hydroxy-Succinimide; PC, Phosphatidylcholine; Pec-8PUH NPs, pectin-eight-arm polyethylene glycol-ursolic acid/hydrooxycampothecin nanoparticle; SPC, Soybean Phosphatidyl Choline; UA-NPs, Ursolic Acid- Nanoparticles; UA-LA-ICG NPs, Ursolic Acid- Lactobionic Acid -Indocyanine Green; UA-PMs, Ursolic Acid-Polymer Micelles; U-SS-M, Micelles assembled by PEG-SS-UA (polyethylene glycol using a disulfide bond)