| chitosan–4-thiobutylamidine |
mice |
nanoparticles |
intravenous delivery of 5-fluorouracil and curcumin |
A
sustained release over 72 h of curcumin
and 5-fluorouracil was achieved
by incorporating these APIs in TC nanoparticles. Furthermore, an 18.8-fold higher AUC was analyzed for 5-fluorouracil
compared to the API solution, and for curcumin a 6.5-fold increased AUC was obtained. |
(232) |
| rats |
microparticles |
nasal insulin delivery |
A bioavailability of 7%
and a calculated absolute pharmacological efficacy of 5% were obtained
for TC. CS displayed a bioavailability of 4% and a pharmacological
efficacy of 0.7%. |
(209) |
| oral acyclovir delivery |
Mean residence time of TC
microparticles was 17.9 h. CS particles
showed only a mean residence time of 12.4 h. Furthermore, a 1.2-fold higher AUC
was obtained for TC microparticles in relation to CS particles. |
(198) |
| polymer tablets |
oral calcitonin delivery |
Delivery system based on
TC decreased the plasma calcium concentration to 91%, whereas control
tablets based on CS had no impact on plasma calcium level. |
(204) |
| oral delivery of P-gp substrates |
Tablets
based on TC increased
the AUC of Rhodamine-123 by 217% in comparison to buffer control and
by 58% compared to CS. |
(203) |
| pigs |
polymer tablets |
buccal pituitary adenylate
cyclase-activating polypeptide delivery |
Delivery system based on
TC led to a bioavailability of 1%, whereas no API was detected in
plasma using CS. |
(159) |
| oral antide delivery |
For the administered solution,
no API was analyzed in plasma. In contrast, for TC tablets, an absolute
bioavailability of 1.1% was obtained. |
(155) |
| |
| chitosan–cysteine |
mice |
hydrogel |
curcumin-containing
formulations
were injected into the breast fat pad |
For the hydrogel composed
of TC-coated liposomes, no tumor recurrence was observed, whereas
unmodified liposomes displayed a recurrence rate of 50%. |
(191) |
| |
| chitosan–glutathione |
rats |
nanoparticles |
oral docetaxel delivery |
Oral bioavailability of
the API was increased to 68.9% for TC nanoparticles compared to 6.5%
for the commercially available reference. Furthermore, for TC nanoparticles,
a drug release for 216 h was observed,
whereas for the commercially available reference product, the release
lasted only for 24 h. |
(63) |
| |
| chitosan–mercaptonicotinic
acid |
mice |
nanoparticles |
oral insulin delivery |
The AUC after oral administration
of TC nanoparticles was 4-fold improved
compared to that of CS nanoparticles. |
(201) |
| nanoparticles |
intramuscular delivery of
pDNA encoding for green fluorescent protein |
Gene expression persisted
up to 60 days. |
(79) |
| rats |
polymer tablets |
oral insulin delivery |
For tablets based on TC,
a 4.8-fold higher AUC was observed
in comparison to those based on CS. |
(43) |
| |
| chitosan–mercaptopropionic
acid |
rats |
nanoparticles |
oral insulin delivery |
An increased insulin concentration
and a decreased glucose level were analyzed for streptozotocin-induced
diabetic rats. |
(200) |
| |
| chitosan–N-acetylcysteine |
rats |
nanoparticles |
nasal insulin delivery |
Intranasal administration
of API-loaded nanoparticles based on TC enhanced the relative bioavailability
of the API (12%) compared with CS nanoparticles (7%) and control insulin
solution (1%). |
(156) |
| rabbits |
nanoparticles |
ocular curcumin delivery |
For TC-coated nanoparticles,
the significantly highest ocular retention was observed by fluorescence
imaging, and a 29.9-fold increased
AUC was obtained compared to that with curcumin eye drops. Uncoated
nanoparticles displayed a 6.0-fold higher
AUC, and for CS-coated nanoparticles a 12.3-fold increased AUC was detected. |
(143) |
| humans |
nanofiber mats |
local oral delivery of Garcinia mangostana extract or α-mangostin for caries prevention |
API-loaded nanofiber mats
based on TC achieved a ≥70% reduction
in Streptococcus spp. and Lactobacillus spp. |
(128, 219) |
| |
| chitosan–thioglycolic
acid |
mice |
nanoparticles |
nasal
theophylline delivery |
Theophylline administered
via TC nanoparticles more strongly attenuated pulmonary inflammation
and epithelial damage as well as goblet cell hyperplasia and resulted
in a lower amount of infiltrated inflammatory cells compared to API
delivery by CS nanoparticles. |
(214) |
| nasal
vaccination with bovine
serum albumin (proof of concept) |
High levels of IgG, IgG1, and IgG2a antibodies were found within the animals,
demonstrating the potential of TC-based carriers for nanovaccines. |
(67) |
| nasal delivery of selegiline |
Animals treated with a system
based on TC showed a significantly reduced immobility time, increased
sucrose water intake, and higher locomotor activity compared to the
group receiving a formulation with unmodified polymer. |
(157) |
| intranasal delivery of plasmid
DNA encoding for green fluorescent protein |
Cross-linked TC/pDNA nanoparticles displayed a significantly higher
transfection efficacy (47%) after 14 days in comparison to particles based on CS (21%). |
(213) |
| rats |
hydrogels |
oral
leuprolide delivery |
Gel formulation based on
TC and CS led to an absolute bioavailability of 283% and 43%, respectively. |
(158) |
| nanoparticles |
oral low-molecular-weight
heparin delivery |
Compared
with nanoparticles
based on CS, the anticoagulant effect was significantly longer (maximal
activated partial thromboplastin time was 2-fold increased) for nanoparticles based on TC. |
(160) |
| oral
docetaxel delivery |
Oral bioavailability was 7.5-fold improved in comparison to DTX suspension. |
(146) |
| oral
sitagliptin delivery |
A 4.7-fold increased efficacy in
lowering plasma glucose concentration was
achieved for TC nanoparticles compared to the API solution. |
(202) |
| nasal leuprolide delivery |
An absolute bioavailability
of 2.6%, 4.3%, or 18.5% was observed by administering the API in solution
or via nanoparticles based on CS or TC, respectively. |
(212) |
| pulmonary calcitonin delivery |
For calcitonin-loaded nanoparticles
based on TC, the hypocalcemic effect lasted for 24 h and a pharmacological availability of 40% was analyzed,
whereas for CS nanoparticles, a hypocalcemic effect of 12 h and pharmacological availability of 27% were
obtained. |
(76) |
| intravesical delivery |
More than 50% of nanoparticles
based on TC remained in the bladder after 6 h, resulting in a 4-fold higher bioadhesion
compared to unmodified CS nanoparticles. |
(226) |
| self-emulsifying
drug delivery
system |
oral insulin
delivery |
TC formulation
displayed
a 3.3-fold higher AUC compared to oral
insulin solution |
(206) |
| |
| chitosan–thioglycolic
acid–6-mercaptonicotinamide |
rats |
liposomes |
oral salmon calcitonin delivery |
Liposomes coated with TC
and S-preactivated TC achieved 5.7-
and 8.2-fold improved decreases in
blood calcium level, respectively, in comparison to the API administered
in solution. |
(91) |
| polymer tablets |
oral antide delivery |
An absolute bioavailability
of 0.03% was observed for CS tablets, which could be increased to
1.4% using TC tablets. |
(151) |
| |
| dimethyl ethyl chitosan–mercaptopropionic
acid |
rabbit |
polymer solution |
ocular dexamethasone delivery |
CS-API solution showed a 3.4-fold higher AUC in comparison to the API solution
without chitosan. For the TC-API solution,
however, a 5.7-fold higher AUC was
found. |
(111) |
| |
| galactosylated
trimethyl-chitosan–cysteine |
mice |
nanoparticles |
oral
delivery of Map4k4
siRNA |
Daily oral
administration
of galactolsylated TC nanoparticles containing siMap4k4 significantly
improved dextrane sulfate sodium-induced ulcerative colitis body weight
loss, colon length shortening, and increase of myeloperoxidase activity. |
(38) |
| |
| hexanoic acid, 6-[(mercapto-1-oxopropyl)amino]chitosan |
mice |
nanoparticles |
oral delivery of TNF-α siRNA |
TC particles
showed high
accumulation at the arthritic joint sites in collagen-induced arthritis
mice, significantly inhibiting inflammation and bone erosion comparable
to methotrexate (5 mg/kg). |
(112) |
| intravenous administration
of VEGF siRNA |
A 34.4%
decreased VEGF expression
in extracted tumor tissue was analyzed for TC nanoparticles in reference
to the control. Moreover, a synergistic effect was obtained by administering
TC nanoparticles together with bevacizumab, as thereby VEGF expression
was reduced by 43.5%. |
(233) |
| |
| mannosylated trimethyl-chitosan–cysteine |
mice |
nanoparticles |
oral delivery of TNF-α siRNA |
Orally delivered
TC nanoparticles
inhibited TNF-α production in
macrophages, protecting mice with acute hepatic injury from inflammation-induced
liver damage and lethality. |
(31) |
| |
|
N-mercaptoacetyl-N′-octyl-O,N″-glycol chitosan |
rats |
micelles |
oral paclitaxel delivery |
TC micelles increased the
bioavailability of paclitaxel to 78%, being 3.8-fold higher compared to the marketed reference product and 1.4-fold higher in relation to micelles based on
CS. |
(80) |
| |
| thiomalylchitosan |
rats |
nanoparticles |
oral insulin delivery |
For insulin-loaded TC nanoparticles,
a 35% reduced blood glucose level was observed, whereas for CS nanoparticles
blood glucose level decreased by 17%. |
(84) |
| |
| trimethyl-chitosan–cysteine |
mice |
nanoparticles |
intramuscular delivery of
pDNA encoding for green fluorescent protein |
Transfection with TC achieved
a 2.3-fold and 4.1-fold higher efficiency than CS and Lipofectamine2000, respectively. |
(34) |
