scholarly journals Cellulose/Exosome Nanocarrier for Improved Prolonged Release of 5-Fluorouracil: Preparation, Characterization, Drug Release Behavior and Cytotoxicity

Author(s):  
Maryam Saeidifar ◽  
Mobina Seyedahmadi ◽  
Jafar Javadpour ◽  
Hamid Reza Rezaei

Abstract Designing of nanoparticle drug delivery systems and improving the efficacy of anticancer drugs are a great deal of effort in the recent years. In this study, a novel biocompatible nanocarrier based on bacterial cellulose (BC) in presence of exosome (Exo) was prepared to controlled release of 5-fluorouracil (5-FU), (5-FU.Exo@BC). The physicochemical properties of 5-FU.Exo@BC was characterized using field emission scanning electron microscopy (FESEM), Differential Scanning Calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), and X-ray Diffraction (XRD) techniques that confirmed the successful preparation of 5-FU.Exo@BC. The release behavior of 5-FU.Exo@BC compared to 5-FU and 5-FU@BC demonstrated a significant sustained release during 162 h. The release mechanism of the above three systems followed Korsmeyer-peppas with non-Fickian diffusion for 5-FU@BC and 5-FU.Exo@BC. In addition, the viability of HT-29 cells (human colon cancer cell line), towards BC, 5-FU@BC and 5-FU.Exo@BC indicated the promising efficacy of 5-FU into 5-FU.Exo@BC. Subsequently, the prepared bio-nanocomposite could be proposed as a potential drug delivery system with effective controlled-release function.

Author(s):  
Dhulipalla Mounika ◽  
I. Deepika Reddy ◽  
K. Sai Chandralekha ◽  
Kapu Harika ◽  
Ramarao Nadendla ◽  
...  

Oral drug delivery is the most widely utilized route of administration among all the routes that have been explored for systemic delivery of drugs via pharmaceutical products of different dosage form. Oral route is considered most natural, uncomplicated, convenient and safe due to its ease of administration, patient acceptance and cost-effective manufacturing process. Gastroretentive drug delivery system was developed in pharmacy field and drug retention for a prolonged time has been achieved. The goal of this study was to formulate and in-vitro evaluate Ciprofloxacin HCl controlled release matrix floating tablets. Ciprofloxacin HCl floating matrix tablets were prepared by wet granulation method using two polymers such as HPMC K100M (hydrophilic polymer) and HPMC K15M. All the Evaluation parameters were within the acceptable limits. FTIR spectral analysis showed that there was no interaction between the drug and polymers. In-vitro dissolution study was carried out using USP dissolution test apparatus (paddle type) at 50 rpm. The test was carried out at 37 ± 0.5 0C in 900ml of the 0.1 N HCl buffer as the medium for eight hours. HPMC K100M shows a prolonged release when compared to HPMC K15M. These findings indicated that HPMC K100M can be used to develop novel gastroretentive controlled release drug delivery systems with the double advantage of controlled drug release at GIT pH. On comparing the major criteria in evaluation such as preformulation and in vitro drug release characteristics, the formulation F8 was selected as the best formulation, as it showed the drug content as 99±0.4% and swelling index ratio was 107.14, and in-vitro drug released 61.31±0.65% up to 8 hours. Results indicated that controlled Ciprofloxacin HCl release was directly proportional to the concentration of HPMC K100M and the release of drug followed non-Fickian diffusion. Based on all the above evaluation parameters it was concluded that the formulation batch F8 was found to be best formulation among the formulations F1 to F8 were prepared.


Author(s):  
Zhenlin Chen ◽  
Fangjian Ning ◽  
Xingcun He ◽  
Hailong Peng ◽  
Hua Xiong

AbstractIn this work, salidroside, a functional food agent, was incorporated into novel interpenetrating polymer network microspheres (IPN-Ms) prepared by chitosan (CS) and methylcellulose (MC) for controlled release and stabilization. IPN-Ms were characterized using scanning electron microscopy, Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry and X-ray diffraction. The result indicated that salidroside-loaded IPN-Ms (S-IPN-Ms) are hollow and highly spherical, with a coarse pleated surface and a particle size ranging from 5 to 30 µm. Schiff base formation and the hemiacetal reaction are the primary mechanisms underlying the interpenetrating network cross-linking of IPN-Ms. In S-IPN-Ms, the CS and MC were homogeneously blended, and the salidroside was molecularly and amorphously dispersed. The encapsulation efficiency of the salidroside within the S-IPN-Ms was up to 75.64 %. In the S-IPN-M complex, the release of salidroside by S-IPN-Ms was governed by burst and sustained release, and Fickian diffusion was the primary release mechanism for the entire release process. Thus, controlled release and stabilization of salidroside were achieved through incorporation of salidroside into IPN-Ms prepared by chitosan (CS) and methylcellulose.


Author(s):  
Yuan Feng ◽  
Xinran Liu ◽  
Yueqing Han ◽  
Mantian Chen ◽  
Lin Zhang ◽  
...  

Background & Objective: Nowadays, the interaction between natural products and microRNAs provides a promising field for exploring the chemo preventive agents for various cancers.As a member of microRNAs, the expression of let-7f-5p is universally down regulated in colorectal cancer (CRC). The present study aimed to uncover the function of let-7f-5p in the proliferation of human colon cancer cell line Caco2 and explored chemo preventive agents from natural resources that can prevent the development of CRC. Methods: Herein, Caco2 cells were transfected with let-7f-5p mimic and inhibitor to manipulate let-7f-5p levels, and the expression of let-7f-5p wasper formed by RT‑qPCR. Next, we determined how let-7f-5p regulates Caco2 cell proliferation by using MTT, wound-healing, cell cycle,and colony formation assays.Besides, to further understand the effect of let-7f-5p, we evaluated the protein level of AMER3 and SLC9A9 by using western blotting assays. Results: The results showed a suppressive function of let-7f-5p on Caco2 cell proliferation and then put forward a triterpenoid (rotundic acid, RA) which significant antagonized the effect of cell proliferation, restitution after wounding,and colony formation caused by let-7f-5p. Moreover, the western blot results further indicated that the inhibitory effect of RA might be due to its suppressive role in let-7f-5p-targeted AMER3 and SLC9A9 regulation. Conclusion: Our validation study results confirmed that let-7f-5p was a potent tumor suppressor gene of Caco2 cell proliferation,and RA showed as a regulator of the effect oflet-7f-5p on cell proliferation and then could be a potential chemo preventive agent for CRC treatment.


Author(s):  
Kailas D. Datkhile ◽  
Satish R. Patil ◽  
Pratik P. Durgawale ◽  
Madhavi N. Patil ◽  
Dilip D. Hinge ◽  
...  

Abstract Background Nanomedicine has evolved as precision medicine in novel therapeutic approach of cancer management. The present study investigated the efficacy of biogenic gold nanoparticles synthesized using Argemone mexicana L. aqueous extract (AM-AuNPs) against the human colon cancer cell line, HCT-15. Results Biosynthesis of AM-AuNPs was determined by ultraviolet-visible spectroscopy and further characterized by transmission electron microscopy, X-ray diffraction, and Fourier transition infrared spectroscopy analysis. The cytotoxic activity of AM-AuNPs was assessed by the 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay, whereas genotoxicity was evaluated by the DNA fragmentation assay. The expression of apoptosis regulatory genes such as p53 and caspase-3 was explored through semi-quantitative reverse transcriptase polymerase chain reaction (RT-PCR) and western blotting to evidence apoptotic cell death in HCT-15 cells. Biogenic AM-AuNPs inhibited cell proliferation in HCT-15 cell line with a half maximal inhibitory concentration (IC50) of 20.53 μg/mL at 24 h and 12.03 μg/mL at 48 h of exposure. The altered cell morphology and increased apoptosis due to AM-AuNPs were also evidenced through nuclear DNA fragmentation and upregulated expression of p53 and caspase-3 in HCT-15 cells. Conclusion The AM-AuNPs may exert antiproliferative and genotoxic effects on HCT-15 cells by cell growth suppression and induction of apoptosis mediated by activation of p53 and caspase-3 genes.


2017 ◽  
Vol 12 (2) ◽  
pp. 4
Author(s):  
Di-Wen Shou ◽  
Yue-Lin Zheng

<p class="Abstract">The primary objective of the current work was to investigate the antitumor potential of <em>Primula macrophylla</em> extracts in human colon cancer cell line (Colo-205) along with evaluating the effects on apoptosis induction, cell cycle arrest and mitochondrial membrane potential. Cell viability was assessed by tetrazolium-based MTT assay. Flow cytometry measurement was carried out to assess the effect of the extract on cell cycle phase distribution and mitochondrial transmembrane potential. Results showed that <em>P.  macrophylla</em> methanol extract was effective and exhibited highest cell growth inhibition (IC<sub>50</sub> value, 26.17 μg/mL). Methanol extract significantly increased the side-scattering profile of Colo-205 cells in concentration-dependent pattern. Exposure of Colo-205 cells with different concentrations of the methanol extract (0-80 μg/mL) caused dose-dependent G0/G1 cell cycle arrest along with inducing apoptotic cascade by increasing the population of cells at G0/G1 phase. Furthermore, methanol extract treatment caused an increase in mitochondrial membrane depolarization in Colo-205 cells.</p><p class="Abstract"><strong>Video Clip of Methodlogy</strong> (3 min 17 sec): <a href="https://youtube.com/v/yy-rCjDN830">Click</a>  <a href="https://youtube.com/watch?v=yy-rCjDN830">If failed</a></p>


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