TY - JOUR
T1 - Venlafaxine loaded chitosan NPs for brain targeting
T2 - Pharmacokinetic and pharmacodynamic evaluation
AU - Haque, Shadabul
AU - Md, Shadab
AU - Fazil, Mohammad
AU - Kumar, Manish
AU - Sahni, Jasjeet Kaur
AU - Ali, Javed
AU - Baboota, Sanjula
PY - 2012/6/5
Y1 - 2012/6/5
N2 - The purpose of the present investigation was to prepare venlafaxine (VLF) loaded chitosan nanoparticles (NPs) to enhance the uptake of VLF to brain via intranasal (i.n.) delivery. VLF loaded chitosan NPs were prepared and characterized for particle size, size distribution, zeta potential, encapsulation efficiency and in vitro drug release. In order to investigate the localization of chitosan NPs in brain and other organs qualitatively confocal laser scanning microscopy technique was carried out using rhodamine-123 (ROD-123) as marker. The levels of VLF in plasma and brain tissues were also determined, the brain/blood ratios of VLF for VLF (i.v.), VLF (i.n.), VLF chitosan NPs (i.n.) were 0.0293, 0.0700 and 0.1612, respectively, at 0.5 h, indicative of better brain uptake of VLF chitosan NPs. The higher drug transport efficiency (508.59) and direct transport percentage (80.34) of VLF chitosan NPs as compared to other formulations suggest its better efficacy in treatment of depression.
AB - The purpose of the present investigation was to prepare venlafaxine (VLF) loaded chitosan nanoparticles (NPs) to enhance the uptake of VLF to brain via intranasal (i.n.) delivery. VLF loaded chitosan NPs were prepared and characterized for particle size, size distribution, zeta potential, encapsulation efficiency and in vitro drug release. In order to investigate the localization of chitosan NPs in brain and other organs qualitatively confocal laser scanning microscopy technique was carried out using rhodamine-123 (ROD-123) as marker. The levels of VLF in plasma and brain tissues were also determined, the brain/blood ratios of VLF for VLF (i.v.), VLF (i.n.), VLF chitosan NPs (i.n.) were 0.0293, 0.0700 and 0.1612, respectively, at 0.5 h, indicative of better brain uptake of VLF chitosan NPs. The higher drug transport efficiency (508.59) and direct transport percentage (80.34) of VLF chitosan NPs as compared to other formulations suggest its better efficacy in treatment of depression.
KW - Biodistribution
KW - Brain targeting
KW - Chitosan
KW - Confocal microscopy
KW - Intranasal route
KW - Venlafaxine
UR - http://www.scopus.com/inward/record.url?scp=84860214736&partnerID=8YFLogxK
U2 - 10.1016/j.carbpol.2012.02.051
DO - 10.1016/j.carbpol.2012.02.051
M3 - Article
C2 - 24750606
AN - SCOPUS:84860214736
VL - 89
SP - 72
EP - 79
JO - Carbohydrate Polymers
JF - Carbohydrate Polymers
SN - 0144-8617
IS - 1
ER -