Approaches for Targeted Drug Delivery to Colon

Author(s):  
Shyam Prasad ◽  
Vidhu Aeri ◽  
Yashwant .

The conventional drug delivery system for colonic disease may leads to absorption of drug across biological membrane of gastrointestinal tract (GIT). The absorption of drug throughout GIT may leads to increase in dose and associated side effects. Colon targeted drug delivery (CTDD) is a method of delivering medication to a patient in a manner that increases concentration of the medication in colon relative to other part of GIT. The aim of CTDD is to prolong, localize, target and have protected drug interaction to diseased tissue. The present review deals with primary as well as recent approaches of delivery of drug to colon.

2021 ◽  
Vol 18 ◽  
Author(s):  
Sumel Ashique ◽  
Navjot Kaur Sandhu ◽  
Viney Chawla ◽  
Pooja A Chawla

Background: Due to various limitations in conventional drug delivery system, it is important to focus on the target-specific drug delivery system where we can deliver the drug without any degradation. Among various challenges faced by a formulation scientist, delivering the drug to its right site, in its right dose, is also an important aim. A focused drug transport aims to extend, localize, target and have a safe drug interaction with the diseased tissue. Objective: The aim of targeted drug delivery is to make the required amount of the drug available at its desired site of action. Drug targeting can be accomplished in a number ways that include enzyme mediation, pH-dependent release, use of special vehicles, receptor targeting among other mechanisms. Intelligently designed targeted drug delivery systems also offer the advantages of a low dose of the drug along with reduced side effects which ultimately improves patient compliance. Incidences of dose dumping and dosage form failure are negligible. A focused drug transport aims to have a safe drug interaction with the diseased tissue. Conclusion: This review focuses on the available targeting techniques for delivery to the colon, brain and other sites of interest. Overall, the article should make an excellent read for the researchers in this area. Newer drug targets may be identified and exploited for successful drug targeting.


Author(s):  
Diksha Sharma ◽  
Abhishek Sharma

  The drug delivery system has been advanced to release the drug according to the body requirement during the entire period of treatment and also for the delivery at the targeted site. Several novel drug delivery systems have emerged encompassing different route of administration to achieve controlled and targeted drug delivery, magnetic microsphere carrier being one of them. Magnetic microsphere is an alternative to traditional radiation methods. As the traditional radiation methods use highly penetrating radiation that is absorbed throughout the body and cause side effects hence its use is limited. Therefore, a safe and effective alternate is needed like magnetic microsphere. The excessive circulating drug particles are minimized by this delivery system. Moreover, the aim of specific targeting is to enhance the effectiveness of drug delivery and at the same time to lessen the toxicity and side effects. Magnetic carriers receive magnetic responses to a magnetic field from incorporated materials that are used for magnetic microsphere are chitosan, dextran, etc. One of the most utilized magnetic microspheres is serum albumine whether from human or other suitable animals. Drug release from the albumin microsphere can be controlled by various stabilization procedures. Overall, the targeted magnetic microsphere is much valuable novel drug delivery system for what more work have to be done. By knowing the importance of all this, the present paper reviews the mechanism, preparation, and applications of magnetic microspheres. As the targeted drug delivery system implies selective and effective localization of drug into the target at therapeutic concentrations with limited access to non-target sites. Magnetic microspheres hold great promises for reaching the goal of controlled and site-specific drug delivery.


Author(s):  
Elahe Darvishi ◽  
Mahsa Minadi ◽  
Somayeh Mirsadeghi ◽  
Behrang Shiri

Introduction: Much research has been carried out to improve drug delivery and targeted drug delivery to the body in order to minimize side effects, provide controlled delivery of the drug to the desired location and to achieve optimal therapeutic effects. Zeolitic imidazolate-8 (ZIF-8) is a subset of MOFs that are biocompatible, stable in the aquatic environment and have adjustable porosity. In addition, at pHs 5 or 6, the bond between imidazolate-zinc ions disappears and releases the drug. In this project, ZIF-8 was used as a curcumin carrier to improve the physicochemical properties and enhance the efficacy of lipophilic drugs in the treatment of cancer. Methods: This research was a basic experimental study. ZIF-8 nanoparticles were fabricated by co-precipitation method. In addition, to prove their pH sensitivity, curcumin was first encapsulated in situ in ZIF-8 and characterized by XRD, SEM, TEM, DLS methods. Then its release was investigated at two pH of five and 7.4 saline phosphate buffer. Finally, In vitro study by MTT assay was performed on prostate cancer cell line (PC3). Data were compared by analysis of variance (ANOVA) using SPSS version 16 software. Results: After characterization of the nanoparticles by the mentioned methods, it was found that the nanoparticle dimensions were between 80-60 nm and the nanoparticle dimensions with curcumin were between 120-110 nm. In addition, in the synthesis of ZIF-8 nanoparticles, %72 of the drug was loaded, which is an acceptable amount. Conclusion: These nanoparticles showed high capacity in the treatment of prostate cancer and minimal damage to healthy cells. It can be said that using this formulation for targeted drug delivery of cancer not only reduces the side effects of anti-cancer drugs but also increases their effectiveness and can also be used to deliver low-soluble or insoluble drugs in biological environments.


Polymers ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 59
Author(s):  
Abeer M. Beagan ◽  
Ahlam A. Alghamdi ◽  
Shatha S. Lahmadi ◽  
Majed A. Halwani ◽  
Mohammed S. Almeataq ◽  
...  

Currently, chemotherapy is an important method for the treatment of various cancers. Nevertheless, it has many limitations, such as poor tumour selectivity and multi-drug resistance. It is necessary to improve this treatment method by incorporating a targeted drug delivery system aimed to reduce side effects and drug resistance. The present work aims to develop pH-sensitive nanocarriers containing magnetic mesoporous silica nanoparticles (MMSNs) coated with pH-responsive polymers for tumour-targeted drug delivery via the folate receptor. 2-Diethyl amino ethyl methacrylate (DEAEMA) was successfully grafted on MMSNs via surface initiated ARGET atom transfer radical polymerization (ATRP), with an average particle size of 180 nm. The end groups of poly (2-(diethylamino)ethyl methacrylate) (PDEAEMA) brushes were converted to amines, followed by a covalent bond with folic acid (FA) as a targeting agent. FA conjugated to the nanoparticle surface was confirmed by X-ray photoelectron spectroscopy (XPS). pH-Responsive behavior of PDEAEMA brushes was investigated by Dynamic Light Scattering (DLS). The nanoparticles average diameters ranged from ca. 350 nm in basic media to ca. 650 in acidic solution. Multifunctional pH-sensitive magnetic mesoporous nanoparticles were loaded with an anti-cancer drug (Doxorubicin) to investigate their capacity and long-circulation time. In a cumulative release pattern, doxorubicin (DOX) release from nano-systems was ca. 20% when the particle exposed to acidic media, compared to ca. 5% in basic media. The nano-systems have excellent biocompatibility and are minimally toxic when exposed to MCF-7, and -MCF-7 ADR cells.


Cancers ◽  
2021 ◽  
Vol 13 (13) ◽  
pp. 3321
Author(s):  
Etienne J. Slapak ◽  
Lily Kong ◽  
Mouad el Mandili ◽  
Rienk Nieuwland ◽  
Alexander Kros ◽  
...  

Pancreatic ductal adenocarcinoma (PDAC) has the worst survival rate of all cancers. This poor prognosis results from the lack of efficient systemic treatment regimens, demanding high-dose chemotherapy that causes severe side effects. To overcome dose-dependent toxicities, we explored the efficacy of targeted drug delivery using a protease-dependent drug-release system. To this end, we developed a PDAC-specific drug delivery system based on mesoporous silica nanoparticles (MSN) functionalized with an avidin–biotin gatekeeper system containing a protease linker that is specifically cleaved by tumor cells. Bioinformatic analysis identified ADAM9 as a PDAC-enriched protease, and PDAC cell-derived conditioned medium efficiently cleaved protease linkers containing ADAM9 substrates. Cleavage was PDAC specific as conditioned medium from leukocytes was unable to cleave the ADAM9 substrate. Protease linker-functionalized MSNs were efficiently capped with avidin, and cap removal was confirmed to occur in the presence of PDAC cell-derived ADAM9. Subsequent treatment of PDAC cells in vitro with paclitaxel-loaded MSNs indeed showed high cytotoxicity, whereas no cell death was observed in white blood cell-derived cell lines, confirming efficacy of the nanoparticle-mediated drug delivery system. Taken together, this research introduces a novel ADAM9-responsive, protease-dependent, drug delivery system for PDAC as a promising tool to reduce the cytotoxicity of systemic chemotherapy.


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