Theranostic nanotechnologies: moving beyond imaging drug localization?

2014 ◽  
Vol 5 (2) ◽  
pp. 97-100 ◽  
Author(s):  
Frank Alexis ◽  
Jeffrey N Anker
Keyword(s):  
2015 ◽  
Vol 59 (5) ◽  
pp. 2479-2487 ◽  
Author(s):  
Keerti Jain ◽  
Ashwni Kumar Verma ◽  
Prabhat Ranjan Mishra ◽  
Narendra Kumar Jain

ABSTRACTThe present study aimed to develop an optimized dendrimeric delivery system for amphotericin B (AmB). Fifth-generation (5.0G) poly(propylene imine) (PPI) dendrimers were synthesized, conjugated with mannose, and characterized by use of various analytical techniques, including Fourier transform infrared spectroscopy (FTIR),1H nuclear magnetic resonance (1H-NMR) spectroscopic analysis, and atomic force microscopy (AFM). Mannose-conjugated 5.0G PPI (MPPI) dendrimers were loaded with AmB and evaluated for drug loading efficiency,in vitrodrug release profile, stability, hemolytic toxicity to human erythrocytes, cytotoxicity to and cell uptake by J774A.1 macrophage cells, antiparasitic activity against intracellularLeishmania donovaniamastigotes,in vivopharmacokinetic and biodistribution profiles, drug localization index, toxicity, and antileishmanial activity. AFM showed the nanometric size of the MPPI dendrimers, with a nearly globular architecture. The conjugate showed a good entrapment efficiency for AmB, along with pH-sensitive drug release. Highly significant reductions in toxicity toward human erythrocytes and macrophage cells, without compromising the antiparasitic activity of AmB, were observed. The dendrimeric formulation of AmB showed a significant enhancement of the parasiticidal activity of AmB toward intramacrophagicL. donovaniamastigotes. In thein vitrocell uptake studies, the formulation showed selectivity toward macrophages, with significant intracellular uptake. Further pharmacokinetic and organ distribution studies elucidated the controlled delivery behavior of the formulation. The drug localization index was found to increase significantly in macrophage-rich organs.In vivostudies showed a biocompatible behavior of MPPIA, with negligible toxicity even at higher doses, and promising antileishmanial activity. From the results, we concluded that surface-engineered dendrimers may serve as optimized delivery vehicles for AmB with enhanced activity and low or negligible toxicity.


2016 ◽  
Vol 11 (9) ◽  
pp. 2541-2550 ◽  
Author(s):  
Anna Rutkowska ◽  
Douglas W. Thomson ◽  
Johanna Vappiani ◽  
Thilo Werner ◽  
Katrin M. Mueller ◽  
...  

1966 ◽  
Vol 44 (2) ◽  
pp. 345-351
Author(s):  
L. Berlinguet ◽  
N. Bégin ◽  
L. Nicole ◽  
A. Ho-Van-Hap ◽  
P. Singh

Autoradiography was used to follow the distribution of 1-aminocyclopentanecarboxylic acid (ACPC), its analogue 1-amino-2-methylcyelopentanecarboxylic acid, tryptamine, and a barbituric acid analogue of phenylalanine. Mice were injected with 14C-labelled compounds, and sagittal sections were exposed for autoradiography. ACPC was localized in the pancreas and also in Walker tumors. Similarly, the methyl analogue accumulated in the pancreas but was located also in the kidney. There was a high content in an Ehrlich ascites tumor. The barbiturate was found mainly in the intestine and gallbladder. Tryptamine was rapidly metabolized and excreted through the kidney. These findings add much to the information obtained by the classical techniques of biochemistry.


2020 ◽  
Vol 13 (8) ◽  
pp. 167 ◽  
Author(s):  
Pratheeksha Koppa Raghu ◽  
Kuldeep K. Bansal ◽  
Pradip Thakor ◽  
Valamla Bhavana ◽  
Jitender Madan ◽  
...  

The topical route is the most preferred one for administering drugs to eyes, skin and wounds for reaching enhanced efficacy and to improve patient compliance. Topical administration of drugs via conventional dosage forms such as solutions, creams and so forth to the eyes is associated with very low bioavailability (less than 5%) and hence, we cannot rely on these for delivering drugs to eyes more efficiently. An intravitreal injection is another popular drug delivery regime but is associated with complications like intravitreal hemorrhage, retinal detachment, endophthalmitis, and cataracts. The skin has a complex structure that serves as numerous physiological barriers to the entry of exogenous substances. Drug localization is an important aspect of some dermal diseases and requires directed delivery of the active substance to the diseased cells, which is challenging with current approaches. Existing therapies used for wound healing are costly, and they involve long-lasting treatments with 70% chance of recurrence of ulcers. Nanotechnology is a novel and highly potential technology for designing formulations that would improve the efficiency of delivering drugs via the topical route. This review involves a discussion about how nanotechnology-driven drug delivery systems have evolved, and their potential in overcoming the natural barriers for delivering drugs to eyes, skin and wounds.


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