Functionalized layer-by-layer assembled film with directional 5-fluorouracil release to target colon cancer

Janardhanam, Leela Sai Lokesh; Indukuri, Vikram Varma; Verma, Pratishtha; Dusane, Apurva Chandrashekhar; Venuganti, Venkata Vamsi Krishna

doi:10.1016/j.msec.2020.111118

Cited by 30 publications

(30 citation statements)

References 29 publications

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“…The cumulative amount of MF released from the chitosan-side was signi cantly (p < 0.0001) greater than the PCL-side. The drug release behavior of 5FU from LbL lm was reported in our earlier publication 37 . A similar observation of restricted drug release from the PCL (backing layer) side was observed for 5FU.…”

Section: Fu and Mf Release Studies From Lbl Lmmentioning

confidence: 82%

“…The chitosan and sodium alginate used in preparing LbL lm are biodegradable and show mucoadhesive property [46][47][48] . The nature of interactions between the entrapped drug and polyelectrolytes in uence the loading e ciency and release behavior from LbL lms 49,50 The mucoadhesive nature of chitosan surface allows adhesion of LbL lm to the colon tissue after release from the Eudragit S100 coated capsule upon oral administration 37,53 . Earlier reports showed directional release of 5FU, oxaliplatin and STAT3 siRNA from LbL lm after adhesion in the colon tissue 13,37 .…”

Section: Discussionmentioning

confidence: 99%

“…In an earlier report, we have demonstrated development of 5FU loaded LbL lm for directional release and colon tissue adhesion 37 . The objective of this study was to perform pharmacokinetic analysis of 5FU loaded LbL lm after oral administration in colon targeted capsule.…”

Section: Introductionmentioning

confidence: 94%

“…Figure 4c and 4f shows characteristic absorbance peaks of 5FU and MF loaded LbL lm after each bilayer deposition. The characteristric FTIR peaks of 5FU appears in the range of 3000-3500, 1600-1820 and 1000-1400 cm -1 corresponding to secondary amide stretching, carbonyl group stretching and C-F bond stretching vibrations, respectively 37 . The 5FU-LbL lm showed all the characteristic peaks, among which the broad peak at 3100-3300 cm 1 was found distinguishable between different bilayers.…”

Section: Characterization Of Lbl Lmmentioning

confidence: 99%

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Colon targeted layer-by-layer self-assembled film: pharmacokinetic analysis of model drugs after oral administration

Janardhanam

Deokar

Bollareddy

et al. 2022

Preprint

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The aim of the study was to investigate the pharmacokinetic parameters of 5-fluorouracil (5FU) and moxifloxacin (MF) after oral administration using layer-by-layer assembled film in enteric coated capsule. The LbL film was prepared by sequential layering of chitosan and sodium alginate polyelectrolytes containing either 5FU or MF. The films were characterized for physical characteristics, drug loading and release behaviour. Pharmacokinetic studies were performed in the rat model for three different drug concentrations after oral administration and compared with intravenous administration. The results showed that the thickness of 10 bilayerd film was 147 ± 11.66 and 212.3 ± 7.19 µm after 5FU and MF loading, respectively. The amount of 5FU and MF loaded was found to be 1.93 ± 0.48 and 4.64 ± 0.33 mg/cm2, respectively. The DSC and PXRD results showed crystalline nature of 5FU and MF after entrapment in LbL film. The LbL film with backing layer provided directional release of 5FU and MF, where 63.81 ± 4.52% and 101.38 ± 5.08%, respectively was released in 24 h. 5FU showed non-linear pharmacokinetics compared with linear pharmacokinetics showed by MF after oral administration. There is a dose dependent increase in Cmax after oral administration of 5FU and MF LbL film. The Tmax was found to be 720 and 840 mins for 5FU and MF after oral administration. The mean residence time and AUC0-t at 45 mg/kg were 871.4 ± 6.45 min and 198.6 ± 5.03 x 103 min. ng/mL and 1267 ± 142.4 min and 1590 ± 55.60 103 min. ng/mL for 5FU and MF, respectively. Biodistribution studies showed significantly (p<0.01) greater disposition of 5FU within colon tissue after administration using oral LbL film. Taken together, colon targeted LbL film can be developed for oral administration of drugs for local and systemic applications.

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Section: Fu and Mf Release Studies From Lbl Lmmentioning

confidence: 82%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 94%

Section: Characterization Of Lbl Lmmentioning

confidence: 99%

See 2 more Smart Citations

Colon targeted layer-by-layer self-assembled film: pharmacokinetic analysis of model drugs after oral administration

Janardhanam

Deokar

Bollareddy

et al. 2022

Preprint

Self Cite

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“…Layer-by-layer (LBL) self-assembled methods was also used to prepare CANPs for oral CRC treatment (Janardhanam et al., 2020 ). This LBL self-assembly method prepares films that greatly improve the high loading efficiency of 5-FU by using polycaprolactone (PCL, 95% w/w) as the backing.…”

Section: Application Of Canps In Colon Cancer Treatmentmentioning

confidence: 99%

Application of chitosan/alginate nanoparticle in oral drug delivery systems: prospects and challenges

et al. 2022

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Oral drug delivery systems (ODDSs) have various advantages of simple operation and few side effects. ODDSs are highly desirable for colon-targeted therapy (e.g. ulcerative colitis and colorectal cancer), as they improve therapeutic efficiency and reduce systemic toxicity. Chitosan/alginate nanoparticles (CANPs) show strong electrostatic interaction between the carboxyl group of alginates and the amino group of chitosan which leads to shrinkage and gel formation at low pH, thereby protecting the drugs from the gastrointestinal tract (GIT) and aggressive gastric environment. Meanwhile, CANPs as biocompatible polymer, show intestinal mucosal adhesion, which could extend the retention time of drugs on inflammatory sites. Recently, CANPs have attracted increasing interest as colon-targeted oral drug delivery system for intestinal diseases. The purpose of this review is to summarize the application and treatment of CANPs in intestinal diseases and insulin delivery. And then provide a future perspective of the potential and development direction of CANPs as colon-targeted ODDSs.

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Mucoadhesive and antifouling Janus polysaccharide film for prevention of colorectal cancer recurrence post‐surgery

Lee,

Seo,

Park

et al. 2024

BMEMat

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Colorectal cancer is one of the most common cancers, and current treatment options include surgery, chemotherapy, and radiation therapy. Most patients undergo surgery, which often requires extensive resection of the colon to prevent recurrence and metastasis of residual malignant tumor cells, leading to postoperative pain and discomfort in daily routines. Although versatile therapeutic patches have been developed to induce tumor apoptosis, achieving both great adhesiveness on the mucus layers of the colon tissue and anti‐cell/tissue adhesion to other surrounding organs remains a challenge. Herein, we report a Janus polysaccharide film comprising two polymers: mussel‐inspired catechol‐conjugated chitosan (Chi‐C) with muco‐adhesiveness, and alginate (Alg) with anti‐adhesion property. The Chi‐C and Alg polymers form a stably entangled bilayer film via electrostatic interactions. The Janus film shows a strong tissue adhesive strength of ∼10 kPa for the Chi‐C layer and weak strength of ∼1 kPa for the Alg layer. Particularly, the Janus film encapsulating an anti‐cancer drug exhibits a directional release profile to the tumor site, which is effective for triggering tumor death in in vivo colorectal tumor resection model. Ultimately, such anti‐cancer material strategies using bilayered structures are promising for advanced tumor therapy.

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Functionalized layer-by-layer assembled film with directional 5-fluorouracil release to target colon cancer

Cited by 30 publications

References 29 publications

Colon targeted layer-by-layer self-assembled film: pharmacokinetic analysis of model drugs after oral administration

Colon targeted layer-by-layer self-assembled film: pharmacokinetic analysis of model drugs after oral administration

Application of chitosan/alginate nanoparticle in oral drug delivery systems: prospects and challenges

Mucoadhesive and antifouling Janus polysaccharide film for prevention of colorectal cancer recurrence post‐surgery

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