PMID- 28181828
OWN - NLM
STAT- MEDLINE
DCOM- 20170403
LR  - 20210709
IS  - 1521-0464 (Electronic)
IS  - 1071-7544 (Print)
IS  - 1071-7544 (Linking)
VI  - 24
IP  - 1
DP  - 2017 Nov
TI  - Synthesis of sericin-based conjugates by click chemistry: enhancement of 
      sunitinib bioavailability and cell membrane permeation.
PG  - 482-490
LID - 10.1080/10717544.2016.1267822 [doi]
AB  - Sericin is a natural protein that has been used in biomedical and pharmaceutical 
      fields as raw material for polypeptide-based drug delivery systems (DDSs). In 
      this paper, it has been employed as pharmaceutical biopolymer for the production 
      of sunitinib-polypeptide conjugate. The synthesis has been carried out by simple 
      click reaction in water, using the redox couple l-ascorbic acid/hydrogen peroxide 
      as a free radical grafting initiator. The bioconjugate molecular weight 
      (50 kDa < Mw < 75 kDa) was obtained by SDS-PAGE, while the spectroscopic 
      characteristics have been studied in order to reveal the presence of grafted 
      sunitinib. In both FT-IR and UV/Vis spectra, signals corresponding to sunitinib 
      functional groups have been identified. Since sunitinib is an anticancer drug 
      characterized by low bioavailability and low permeability, the bioconjugation 
      aimed at their enhancement. In vitro studies demonstrated that bioavailability 
      has been increased to almost 74%, compared with commercial formulation. Also cell 
      membrane permeability has been augmented in in vitro tests, in which membrane 
      models have been used to determine the lipid membrane/physiological fluid 
      partition coefficient (Kp). The log(Kp) value of the bioconjugate was increased 
      to over 4. This effect resulted in a three-fold decrease of IC(50) value against 
      MCF-7 cells.
FAU - Scrivano, Luca
AU  - Scrivano L
AD  - a Department of Pharmacy, Health and Nutritional Sciences, University of Calabria 
      , Rende , CS , Italy.
FAU - Iacopetta, Domenico
AU  - Iacopetta D
AD  - a Department of Pharmacy, Health and Nutritional Sciences, University of Calabria 
      , Rende , CS , Italy.
FAU - Sinicropi, Maria Stefania
AU  - Sinicropi MS
AD  - a Department of Pharmacy, Health and Nutritional Sciences, University of Calabria 
      , Rende , CS , Italy.
FAU - Saturnino, Carmela
AU  - Saturnino C
AD  - b Department of Sciences, University of Basilicata , Potenza , Italy , and.
FAU - Longo, Pasquale
AU  - Longo P
AD  - c Department of Chemistry and Biology, University of Salerno , Fisciano , SA , 
      Italy.
FAU - Parisi, Ortensia Ilaria
AU  - Parisi OI
AD  - a Department of Pharmacy, Health and Nutritional Sciences, University of Calabria 
      , Rende , CS , Italy.
FAU - Puoci, Francesco
AU  - Puoci F
AD  - a Department of Pharmacy, Health and Nutritional Sciences, University of Calabria 
      , Rende , CS , Italy.
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PL  - England
TA  - Drug Deliv
JT  - Drug delivery
JID - 9417471
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Drug Carriers)
RN  - 0 (Indoles)
RN  - 0 (Protein Kinase Inhibitors)
RN  - 0 (Pyrroles)
RN  - 0 (Sericins)
RN  - V99T50803M (Sunitinib)
SB  - IM
MH  - Antineoplastic Agents/administration & dosage/chemistry/*metabolism
MH  - Biological Availability
MH  - *Cell Membrane Permeability
MH  - Cell Survival/drug effects
MH  - *Click Chemistry
MH  - Dose-Response Relationship, Drug
MH  - *Drug Carriers
MH  - Drug Compounding
MH  - Female
MH  - HeLa Cells
MH  - Humans
MH  - Indoles/administration & dosage/chemistry/*metabolism
MH  - Inhibitory Concentration 50
MH  - Protein Kinase Inhibitors/administration & dosage/chemistry/*metabolism
MH  - Pyrroles/administration & dosage/chemistry/*metabolism
MH  - Sericins/*chemical synthesis
MH  - Solubility
MH  - Spectrophotometry, Ultraviolet
MH  - Spectroscopy, Fourier Transform Infrared
MH  - Sunitinib
MH  - Technology, Pharmaceutical/methods
MH  - Uterine Cervical Neoplasms/*drug therapy/metabolism/pathology
PMC - PMC8240991
OTO - NOTNLM
OT  - Sericin
OT  - bioavailability
OT  - bioconjugates
OT  - cell permeability
OT  - radical grafting
OT  - sunitinib
EDAT- 2017/02/10 06:00
MHDA- 2017/04/04 06:00
PMCR- 2017/02/09
CRDT- 2017/02/10 06:00
PHST- 2017/02/10 06:00 [entrez]
PHST- 2017/02/10 06:00 [pubmed]
PHST- 2017/04/04 06:00 [medline]
PHST- 2017/02/09 00:00 [pmc-release]
AID - 1267822 [pii]
AID - 10.1080/10717544.2016.1267822 [doi]
PST - ppublish
SO  - Drug Deliv. 2017 Nov;24(1):482-490. doi: 10.1080/10717544.2016.1267822.