MAIN FACTORS FOR NANO BASED DELIVERY SYSTEMS
There are two main governing factors for the
nanoparticle based delivery systems: particle size and surface charge.
4. 1. Particle size
Drug loading
and its release is affected by particle size distribution (112). Higher
intracellular uptake of nanoparticles has been recorded compared to micron
sized particles. Nanoparticles can access wide collection of biological targets
because of their tiny size and mobility (113). Delivery and distribution
experiments have suggested that nanoparticles greater than 230 nm size can
congregate in the organ especially in spleen due to the capillary size of this
organ (113). Several in vitro studies have pointed out that particle
size can also control the cellular uptake of nanoparticles (114, 115). Further,
it has been found that particle size is significant for oral drug delivery (113,116).
Topical application to the eye is the well established route (113,256). However, it has been found that small size
differences may be of influence for the actual distribution and bioavailability
(113,225).
Smaller
nonoparticle has more surface area. So, the majority of the drug associated
would close to the exterior part leading to rapid drug release (117). The large
surface area causes the active ingredient to be coupled with in or near the
particle exterior part, and this result in faster active ingredient release
(117).
4. 2. Surface charge
Surface charge is another important
nanoparticle drug delivery system property that can affect the outcome of
particles. Surface charge of gold nanoparticles with PEG caused efficient
internalization in endosomes and cytosol (118). Poly (DL-lactide-co-glycolide)
nanoparticles were found to be ingested by cells by endocytosis (119, 120). It
is found that after entering, the nanoparticles get away from these endosomes
into the cellular cytoplasm. This depends upon the change in surface charge
especially from negative to positive (eg. the PLGA NP resulting in cytoplasmic
delivery). It is hypothesized that the positive surface charge influences the
escape of these nanoparticles from endosomes (119).
The blood-brain barrier (BBB) is an
electrostatic barrier to boundary brain penetration of therapeutics. It has
been reported that nanoparticle surface charge can alter blood-brain barrier
permeability (121). When the particles are absorbed in the blood, their surface
hydrophobicity is related with the amount of adsorbed blood components (122).
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