A seminar on Brain targetted delivery system has been presented here. Role of nanoparticles in such above mentioned drug delivery system is also menitoned here.

1. Submitted By :- Kumar Kapinjal Dev
M.Pharm (Pharmaceutics)

2. • Drug Delivery to the brain includes the process of
passing therapeutically active agents across the blood
brain barrier to treat
the brain disorders. It is a complex process.
• These system provides extended or controlled
release of drugs & protection from degradation.
• Conjugation of drugs is done in the form of
liposomes or Nanoparticles.

3. • The Blood-brain barrier is highly selective
permeable barrier that separates the circulating blood
from the ECF in CNS.
Functions:-
(A).The Blood-brain barrier is composed of highly density
cells that limits the penetration of harmful
substances.
(B). Protects the brain from many infections.
(C). Allows some antibiotics & phagocytes to move
across the BBB.

4. • Microvascular endothelium,
basement membrane & glial
cells such as astrocytes &
pericytes works together to
form BBB.
• Capillaries of brain are linked
with layer of special endothelial
cells that are sealed with tight
junctions.
• BBB holds many transport
proteins for permeation of
molecules. Such as GLUT.

5. • To Treat Glioblastomas :-
They are one of the most common brain tumors.
They are also used to prevent secondary glioblastomas.
• To Treat :- Treating HIV encephalopathy,
epilepsy, neurodegenerative disorders,
Cerebovascular disorders & toxicity.
• To Identify new brain drug targeting system.

6. • Nanoparticles are submicron sized colloidal particles of
size 1 to 1000nm composed of polymer.
• Due to small size nanoparticles penetrates to small
capillaries & allow efficient drug accumulation at the
targeted sites in the body.
• Retention (↑) of nanoparticles with the blood
capillaries results adsorption(↑) due to higher
concentration gradient.
• Some commonly used nanoparticles are derived from:-
Polyalkylcyano acrylates & Polyacetates.

7.  The nanoparticles lead to opening of the tight
junctions between the brain endothelial cells
& the drug permeate through the tight junction.
 Drug loaded nanoparticles could be transcytosed
through endothelial layers.
 Surfactant effect of nanoparticles causes solubilization of
endothelial cell membrane & enhance drug permeability.

8. (A). PEG coated Nanoparticles :-
• It acts as potential hydrophilic cover for hydrophobic
Nanoparticles to increase aqueous
solubility.
• PEG allows Nanoparticles to cross the BBB by interacting
with proteins such as apolipoprotein E.
• It shows promising result in gene therapies.
• PEG complexed nanoparticles are therapauticaly
useful in treating multiple sclerosis &Parkinson’s
disease.

9.  HSA is one of the common proteins found in the
blood.
 Nanoparticles when enters systemic circulation are
commonly surrounded by protein coat mainly composed of
albumin.
 Albumin & albumin coated nanoparticles are able
to release doxorubicin in in vitro neuroblastoma
cell.

10.  Glutathione is an oxidant that protects cells from
toxins produced through oxidative stress.
 PLGA nanoparticles coated with glutathione & loaded with
paclitaxel inhibits cancerous cell growth by inducing
cytotoxicity.
(D). Transferin coated nanoparticles :-
 PLGA nanoparticles coated with transferin loaded with
doxorubicin & paclitaxel shows enhanced inhibition of
tumors.
 They are very appealing in delivering drugs across BBB.

11.  Coating nanoparticles with polysorbate 80 is a popular
method to induce transport across BBB.
 It interacts with apolipoproteins B,E & transported into
endothelial cells by receptor mediated endocytosis.
 IV injection of doxorubicin loaded with PS80 coated
nanoparticles were found to be present in brain after 2
hours of injection.

12. Serial No. Brand Name API Role
1 Ambisome Amphotericin B Liposome for
injections.
2 Caelyx PEGlyated
Liposomal
doxorubicin HCL
Brain tumor
3 Auroshell Gold coated
silica
nanopartciles.
Solid Tumor

13. THANK YOU….