PMID- 26852126
OWN - NLM
STAT- MEDLINE
DCOM- 20170621
LR  - 20220318
IS  - 1432-1955 (Electronic)
IS  - 0932-0113 (Linking)
VI  - 115
IP  - 5
DP  - 2016 May
TI  - Ivermectin-loaded lipid nanocapsules: toward the development of a new 
      antiparasitic delivery system for veterinary applications.
PG  - 1945-53
LID - 10.1007/s00436-016-4937-1 [doi]
AB  - Ivermectin (IVM) is probably one of the most widely used antiparasitic drugs 
      worldwide, and its efficacy is well established. However, slight differences in 
      formulation may change the plasma kinetics, the biodistribution, and in 
      consequence, the efficacy of this compound. The present study focuses on the 
      development of a novel nanocarrier for the delivery of lipophilic drugs such as 
      IVM and its potential application in antiparasitic control. Lipid nanocapsules 
      (LNC) were prepared by a new phase inversion procedure and characterized in terms 
      of size, surface potential, encapsulation efficiency, and physical stability. A 
      complement activation assay (CH50) and uptake experiments by THP-1 macrophage 
      cells were used to assess the stealth properties of this nanocarrier in vitro. 
      Finally, a pharmacokinetics and biodistribution study was carried out as a proof 
      of concept after subcutaneous (SC) injection in a rat model. The final IVM-LNC 
      suspension displayed a narrow size distribution and an encapsulation rate higher 
      than 90 % constant over the evaluated time (60 days). Through flow cytometry and 
      blood permanence measurements, it was possible to confirm the ability of these 
      particles to avoid the macrophage uptake. Moreover, the systemic disposition of 
      IVM in the LNC administered by the SC route was higher (p < 0.05) (1367 ng h/ml) 
      compared to treatment with a commercial formulation (CF) (1193 ng.h/ml), but no 
      significant differences in the biodistribution pattern were found. In conclusion, 
      this new carrier seems to be a promising therapeutic approach in antiparasitic 
      control and to delay the appearance of resistance.
FAU - Gamboa, G V Ullio
AU  - Gamboa GV
AD  - Unidad de Investigacion y Desarrollo en Tecnologia Farmaceutica, UNITEFA-CONICET, 
      Ciudad Universitaria, 5000, HUA, Cordoba, Argentina.
AD  - Departamento de Farmacia, Facultad de Ciencias Quimicas, Universidad Nacional de 
      Cordoba, Ciudad Universitaria, 5000, HUA, Cordoba, Argentina.
FAU - Palma, S D
AU  - Palma SD
AD  - Unidad de Investigacion y Desarrollo en Tecnologia Farmaceutica, UNITEFA-CONICET, 
      Ciudad Universitaria, 5000, HUA, Cordoba, Argentina.
AD  - Departamento de Farmacia, Facultad de Ciencias Quimicas, Universidad Nacional de 
      Cordoba, Ciudad Universitaria, 5000, HUA, Cordoba, Argentina.
FAU - Lifschitz, A
AU  - Lifschitz A
AD  - Laboratorio de Farmacologia, Centro de Investigacion Veterinaria de Tandil, 
      CIVETAN (CONICET), Fac.Cs. Veterinarias, UNCPBA, Tandil, Argentina.
FAU - Ballent, M
AU  - Ballent M
AD  - Laboratorio de Farmacologia, Centro de Investigacion Veterinaria de Tandil, 
      CIVETAN (CONICET), Fac.Cs. Veterinarias, UNCPBA, Tandil, Argentina.
FAU - Lanusse, C
AU  - Lanusse C
AD  - Laboratorio de Farmacologia, Centro de Investigacion Veterinaria de Tandil, 
      CIVETAN (CONICET), Fac.Cs. Veterinarias, UNCPBA, Tandil, Argentina.
FAU - Passirani, C
AU  - Passirani C
AD  - LUNAM Universite, Universite d'Angers, INSERM U1066, IBS-CHU, Angers, 4 rue 
      Larrey, 49933, Angers, France.
FAU - Benoit, J P
AU  - Benoit JP
AD  - LUNAM Universite, Universite d'Angers, INSERM U1066, IBS-CHU, Angers, 4 rue 
      Larrey, 49933, Angers, France.
FAU - Allemandi, D A
AU  - Allemandi DA
AD  - Unidad de Investigacion y Desarrollo en Tecnologia Farmaceutica, UNITEFA-CONICET, 
      Ciudad Universitaria, 5000, HUA, Cordoba, Argentina. dalemand@gmail.com.
AD  - Departamento de Farmacia, Facultad de Ciencias Quimicas, Universidad Nacional de 
      Cordoba, Ciudad Universitaria, 5000, HUA, Cordoba, Argentina. dalemand@gmail.com.
LA  - eng
PT  - Journal Article
DEP - 20160206
PL  - Germany
TA  - Parasitol Res
JT  - Parasitology research
JID - 8703571
RN  - 0 (Antiparasitic Agents)
RN  - 0 (Drug Carriers)
RN  - 0 (Lipids)
RN  - 0 (Nanocapsules)
RN  - 70288-86-7 (Ivermectin)
SB  - IM
MH  - Animals
MH  - Antiparasitic Agents/*therapeutic use
MH  - Drug Administration Routes
MH  - Drug Carriers
MH  - Injections, Subcutaneous
MH  - Ivermectin/*administration & dosage/blood/pharmacokinetics
MH  - Lipids/*chemistry
MH  - Macrophages/metabolism
MH  - Nanocapsules/*chemistry
MH  - Rats
MH  - Tissue Distribution
OTO - NOTNLM
OT  - Drug delivery systems
OT  - Ivermectin
OT  - Lipid nanocapsules
OT  - Pharmacokinetic
OT  - Tissue distribution
EDAT- 2016/02/08 06:00
MHDA- 2017/06/22 06:00
CRDT- 2016/02/08 06:00
PHST- 2015/10/07 00:00 [received]
PHST- 2016/01/20 00:00 [accepted]
PHST- 2016/02/08 06:00 [entrez]
PHST- 2016/02/08 06:00 [pubmed]
PHST- 2017/06/22 06:00 [medline]
AID - 10.1007/s00436-016-4937-1 [pii]
AID - 10.1007/s00436-016-4937-1 [doi]
PST - ppublish
SO  - Parasitol Res. 2016 May;115(5):1945-53. doi: 10.1007/s00436-016-4937-1. Epub 2016 
      Feb 6.