title: Preparation, physicochemical characterization, and cell viability evaluation of long-circulating and pH-sensitive liposomes containing ursolic acid.
abstract: Cancer is one of the leading causes of death worldwide. Although several drugs are used clinically, some tumors either do not respond or are resistant to the existing pharmacotherapy, thus justifying the search for new drugs. Ursolic acid (UA) is a triterpene found in different plant species that has been shown to possess significant antitumor activity. However, UA presents a low solubility in aqueous medium, which presents a barrier to its biological applications. In this context, the use of liposomes presents a promising strategy to deliver UA and allow for its intravenous administration. In this work, long-circulating and pH-sensitive liposomes containing UA (SpHL-UA) were developed, and their chemical and physicochemical properties were evaluated. SpHL-UA presented adequate properties, including a mean diameter of 191.1 ± 6.4 nm, a zeta potential of 1.2 ± 1.4 mV, and a UA entrapment of 0.77 ± 0.01 mg/mL. Moreover, this formulation showed a good stability after having been stored for 2 months at 4 °C. The viability studies on breast (MDA-MB-231) and prostate (LNCaP) cancer cell lines demonstrated that SpHL-UA treatment significantly inhibited cancer cell proliferation. Therefore, the results of the present work suggest the applicability of SpHL-UA as a new and promising anticancer formulation.
authors.affiliation: Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Avenida Antônio Carlos 6627, 31270-901 Belo Horizonte, MG, Brazil.
authors.forename: Sávia
authors.initials: S
authors.lastname: Caldeira de Araújo Lopes
authors.forename: Marcus
authors.initials: M
authors.lastname: Vinícius Melo Novais
authors.forename: Cláudia
authors.initials: C
authors.lastname: Salviano Teixeira
authors.forename: Kinulpe
authors.initials: K
authors.lastname: Honorato-Sampaio
authors.forename: Márcio
authors.initials: M
authors.lastname: Tadeu Pereira
authors.forename: Lucas Antônio Miranda
authors.initials: LA
authors.lastname: Ferreira
authors.forename: Fernão Castro
authors.initials: FC
authors.lastname: Braga
authors.forename: Mônica
authors.initials: M
authors.lastname: Cristina Oliveira
mesh_terms: D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D055598:Chemical Phenomena; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D006801:Humans; D006863:Hydrogen-Ion Concentration / Q000187:drug effects; D020128:Inhibitory Concentration 50; D008081:Liposomes / Q000737:chemistry* / Q000648:ultrastructure; D008297:Male; D010316:Particle Size; D014315:Triterpenes / Q000737:chemistry* / Q000494:pharmacology*; D000097245:Ursolic Acid
chemical_list: D004337:Drug Carriers; D008081:Liposomes; D014315:Triterpenes; D000097245:Ursolic Acid