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Design and development of ligand-appended polysaccharidic nanoparticles for the delivery of oxaliplatin in colorectal cancer  Anekant Jain, MPharm, Sanjay.

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Presentation on theme: "Design and development of ligand-appended polysaccharidic nanoparticles for the delivery of oxaliplatin in colorectal cancer  Anekant Jain, MPharm, Sanjay."— Presentation transcript:

1 Design and development of ligand-appended polysaccharidic nanoparticles for the delivery of oxaliplatin in colorectal cancer  Anekant Jain, MPharm, Sanjay K. Jain, PhD, N. Ganesh, PhD, Jaya Barve, MSc, Aadil M. Beg, BUMS  Nanomedicine: Nanotechnology, Biology and Medicine  Volume 6, Issue 1, Pages (February 2010) DOI: /j.nano Copyright © 2010 Elsevier Inc. Terms and Conditions

2 Figure 1 Mechanistic scheme of colon-specific targeting of Eudragit-coated pellets encapsulating nanoparticles (arbitrary scale). Nanomedicine: Nanotechnology, Biology and Medicine 2010 6, DOI: ( /j.nano ) Copyright © 2010 Elsevier Inc. Terms and Conditions

3 Figure 2 Photomicrographs of chitosan nanoparticles. (A) SEM analysis and (B) TEM analysis of uncoupled nanoparticles. (C) TEM analysis of HA-coupled nanoparticles. Nanomedicine: Nanotechnology, Biology and Medicine 2010 6, DOI: ( /j.nano ) Copyright © 2010 Elsevier Inc. Terms and Conditions

4 Figure 3 Formulations with different ratios of nanoparticles (NP) and HA were prepared. (A) Incubation time optimization for coupling of HA at 25°C. (B) Optimization of total NP/HA weight ratio (zeta potential values after time period of 24 hours at 25°C). All values are expressed as mean ± SD (n = 4). Nanomedicine: Nanotechnology, Biology and Medicine 2010 6, DOI: ( /j.nano ) Copyright © 2010 Elsevier Inc. Terms and Conditions

5 Figure 4 FT-IR spectra of (A) L-OHP, (B) chitosan, (C) drug-bearing uncoupled nanoparticles, and (D) HA-coupled drug-bearing nanoparticles. Nanomedicine: Nanotechnology, Biology and Medicine 2010 6, DOI: ( /j.nano ) Copyright © 2010 Elsevier Inc. Terms and Conditions

6 Figure 5 DSC curve of (A) L-OHP, (B) HA, (C) HA with drug-polymer mixture, and (D) L-OHP–loaded HA-conjugated HACTNPOP formulations, (E) L-OHP–loaded HACTNPOP formulations after storage at 40°C and 75% relative humidity for 6 months. Nanomedicine: Nanotechnology, Biology and Medicine 2010 6, DOI: ( /j.nano ) Copyright © 2010 Elsevier Inc. Terms and Conditions

7 Figure 6 XRDs of (A) L-OHP, (B) blank nanoparticles (HACTNPs), (C) L-OHP–loaded HACTNPOPs, and (D) L-OHP–loaded HACTNPOPs after storage at 40°C and 75% relative humidity for 6 months. Nanomedicine: Nanotechnology, Biology and Medicine 2010 6, DOI: ( /j.nano ) Copyright © 2010 Elsevier Inc. Terms and Conditions

8 Figure 7 In vitro drug release profile of nanoparticulate pellets (HACTNPOEPs and CTNPOEPs) in different simulated fluids. SCF, simulated colon fluid; SGF, simulated gastric fluid; SIF, simulated intestinal fluid. Results are presented as mean ± SD, n = 4. Nanomedicine: Nanotechnology, Biology and Medicine 2010 6, DOI: ( /j.nano ) Copyright © 2010 Elsevier Inc. Terms and Conditions

9 Figure 8 Distribution profiles of free drug and of uncoupled nanoparticles and HA-coupled nanoparticles bearing L-OHP in various tissues as a function of time after oral dose (10 mg/kg) to mice. (A) Pellets of free L-OHP; (B) CTNPOEPs; (C) HACTNPOEPs. represent mean ± SD obtained from two animals per time point. Colon (+C)⁎, includes colon contents and tissue, cecal contents, and tissue; OXA, oxaliplatin; SI, small intestine. Nanomedicine: Nanotechnology, Biology and Medicine 2010 6, DOI: ( /j.nano ) Copyright © 2010 Elsevier Inc. Terms and Conditions

10 Figure 9 γ-scintigraphs captured at different time intervals. (A) Just after administration of pellet showing integrity of the system in stomach. (B) At 1 hour showing the presence of intact enteric-coated pellet in stomach. (C) At 3 hours showing the enteric-coated pellet in small intestine. (D) At 6 hours showing the release of tracer in ascending colon from enteric-coated pellet. (E) At 10 hours showing the release of tracer in ascending colon and entry of pellet mass into transverse colon. (F) At 18 hours showing the distribution of liberated radioactivity in whole colon from enteric-coated pellet. (G) At 24 hours showing the radioactivity in distal part of colon from enteric-coated pellet. Nanomedicine: Nanotechnology, Biology and Medicine 2010 6, DOI: ( /j.nano ) Copyright © 2010 Elsevier Inc. Terms and Conditions


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