PMID- 22687542
OWN - NLM
STAT- MEDLINE
DCOM- 20121022
LR  - 20190720
IS  - 1347-5215 (Electronic)
IS  - 0918-6158 (Linking)
VI  - 35
IP  - 6
DP  - 2012
TI  - Preparation and in vivo evaluation of liposomal everolimus for lung carcinoma and 
      thyroid carcinoma.
PG  - 975-9
AB  - Everolimus has demonstrated antitumor efficacy for various cancers as a result of 
      its inhibition of the mammalian target of rapamycin (mTOR) signaling cascade, 
      which activates cell growth and cell proliferation. However, the low water 
      solubility and low bioavailability of everolimus have prevented its clinical 
      development as an anticancer drug. Therefore, to address the unsuitable 
      characteristic of everolimus, we attempted to prepare liposomal everolimus as a 
      viable drug delivery system, and then evaluated the anticancer efficacy of this 
      system against a medullary thyroid carcinoma cell line (TT cells), a breast 
      cancer cell line (MCF-7 cells) and a small lung carcinoma cell line (NCI-H446 
      cells). The particle size and entrapment efficacy of liposomal everolimus was ca. 
      80 nm and more than 90%, respectively. Liposomal everolimus showed higher 
      cytotoxicity against NCI-H446 cells compared with TT cells. Against NCI-H446 
      tumors, significant suppression of the tumor volume was observed in liposomal 
      everolimus-treated mice by intravenous injection, compared with free 
      everolimus-treated mice by intraperitoneal injection, at a dose of 5 mg/kg 
      without body weight loss. This study showed that liposomal everolimus could be a 
      powerful formulation with anticancer efficacy for some cancers.
FAU - Iwase, Yuko
AU  - Iwase Y
AD  - Institute of Medicinal Chemistry, Hoshi University, Shinagawa-ku, Tokyo, Japan.
FAU - Maitani, Yoshie
AU  - Maitani Y
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Japan
TA  - Biol Pharm Bull
JT  - Biological & pharmaceutical bulletin
JID - 9311984
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Immunosuppressive Agents)
RN  - 0 (Liposomes)
RN  - 7673326042 (Irinotecan)
RN  - 9HW64Q8G6G (Everolimus)
RN  - W36ZG6FT64 (Sirolimus)
RN  - XT3Z54Z28A (Camptothecin)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents/*administration & dosage
MH  - Camptothecin/administration & dosage/analogs & derivatives
MH  - Carcinoma, Small Cell/*drug therapy/pathology
MH  - Cell Line, Tumor
MH  - Cell Survival/drug effects
MH  - Everolimus
MH  - Female
MH  - Humans
MH  - Immunosuppressive Agents/*administration & dosage
MH  - Irinotecan
MH  - Liposomes
MH  - Lung Neoplasms/*drug therapy/pathology
MH  - Mice
MH  - Mice, Inbred BALB C
MH  - Sirolimus/administration & dosage/*analogs & derivatives
MH  - Thyroid Neoplasms
MH  - Tumor Burden/drug effects
MH  - Xenograft Model Antitumor Assays
EDAT- 2012/06/13 06:00
MHDA- 2012/10/23 06:00
CRDT- 2012/06/13 06:00
PHST- 2012/06/13 06:00 [entrez]
PHST- 2012/06/13 06:00 [pubmed]
PHST- 2012/10/23 06:00 [medline]
AID - DN/JST.JSTAGE/bpb/35.975 [pii]
AID - 10.1248/bpb.35.975 [doi]
PST - ppublish
SO  - Biol Pharm Bull. 2012;35(6):975-9. doi: 10.1248/bpb.35.975.