title: Enhanced anticancer potential of encapsulated solid lipid nanoparticles of TPD: a novel triterpenediol from Boswellia serrata.
abstract: A pentacyclic triterpenediol (TPD) from Boswellia serrata has significant cytotoxic and apoptotic potential in a large number of human cancer cell lines. To enhance its anticancer potential, it was successfully formulated into solid lipid nanoparticles (SLNs) by the microemulsion method with 75% drug entrapment efficiency. SEM and TEM studies indicated that TPD-SLNs were regular, solid, and spherical particles in the range of 100-200 nm, and the system indicated that they were more or less stable upon storing up to six months. TPD loaded SLNs showed significantly higher cytotoxic/antitumor potential than the parent drug. TPD-SLNs have 40-60% higher cytotoxic and apoptotic potential than the parent drug in terms of IC(50), extent of apoptosis, DNA damage, and expression of pro-apoptotic proteins like TNF-R1, cytochrome-c, and PARP cleavage in HL-60 cells. Moreover, blank SLNs did not have any cytotoxic effect on the cancer as well as in normal mouse peritoneal macrophages. The in vivo antitumor potential of TPD-SLNs was significantly higher than that of TPD alone in Sarcoma-180 solid tumor bearing mice. Therefore, SLNs of TPD successfully increased the apoptotic and anticancer potential of TPD at comparable doses (both in vitro and in vivo). This work provides new insight into improvising the therapeutic efficacy of TPD by adopting novel delivery strategies such as solid lipid nanoparticles.
authors.affiliation: Indian Institute of Integrative Medicine, CSIR, Canal Road, Jammu 180001, India. sbhushan@iiim.ac.in
authors.forename: Shashi
authors.initials: S
authors.lastname: Bhushan
authors.forename: Vandita
authors.initials: V
authors.lastname: Kakkar
authors.forename: Harish Chandra
authors.initials: HC
authors.lastname: Pal
authors.forename: Santosh Kumar
authors.initials: SK
authors.lastname: Guru
authors.forename: Ajay
authors.initials: A
authors.lastname: Kumar
authors.forename: D M
authors.initials: DM
authors.lastname: Mondhe
authors.forename: P R
authors.initials: PR
authors.lastname: Sharma
authors.forename: Subhash Chandra
authors.initials: SC
authors.lastname: Taneja
authors.forename: Indu Pal
authors.initials: IP
authors.lastname: Kaur
authors.forename: Jaswant
authors.initials: J
authors.lastname: Singh
authors.forename: A K
authors.initials: AK
authors.lastname: Saxena
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry*; D017209:Apoptosis / Q000187:drug effects; D051017:Apoptosis Regulatory Proteins / Q000378:metabolism; D029743:Boswellia / Q000737:chemistry*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D045304:Cytochromes c / Q000378:metabolism; D004249:DNA Damage / Q000187:drug effects; D004655:Emulsions / Q000737:chemistry / Q000494:pharmacology; D018922:HL-60 Cells; D006801:Humans; D008055:Lipids / Q000008:administration & dosage*; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D010316:Particle Size; D053978:Pentacyclic Triterpenes / Q000008:administration & dosage* / Q000737:chemistry*; D010936:Plant Extracts / Q000008:administration & dosage / Q000737:chemistry; D011065:Poly(ADP-ribose) Polymerases / Q000378:metabolism; D012510:Sarcoma 180 / Q000188:drug therapy / Q000378:metabolism; D053199:TNF Receptor-Associated Death Domain Protein / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D051017:Apoptosis Regulatory Proteins; D004655:Emulsions; D008055:Lipids; D053978:Pentacyclic Triterpenes; D010936:Plant Extracts; D053199:TNF Receptor-Associated Death Domain Protein; D045304:Cytochromes c; D011065:Poly(ADP-ribose) Polymerases