Abstract
Background: 6-MP has short elimination time (<2 h) and low bioavailability (~ 50%). Present study was aimed to develop time controlled and site targeted delivery of 6-Mercaptopurine (6-MP) for treatment of colon diseases.
Methods: Compression coating technique was used. 32 full factorial design was designed for optimization of the outer coat for the core tablet. For outer coat amount of Eudragit RS 100 and hydroxypropyl methylcellulose (HPMC K100) were employed as independent variables each at three levels while responses evaluated were swelling index and bursting time. Direct compression method was used for tablets formulation.
Results: 80% w/w of microcrystalline cellulose and 20% w/w of croscarmellose sodium were found to be optimum concentration for the core tablet. The outer coat of optimized batch (ED) contains 21.05% w/w Eudragit RS 100 and 78.95% w/w HPMC K100 of total polymer weight. In-vitro dissolution study indicated that combination of polymer retards the drug release in gastric region and releases ≥95% of drug in colonic region after ≥7 h. Whereas in case of in-vivo placebo x-ray imaging study had shown that the tablet reaches colonic part after 5±0.5 h providing the proof of arrival in the colon. Stability study indicated that the optimized formulation were physically and chemically stable.
Conclusion: Present research work concluded that compression coating by Eudragit RS 100 and HPMC K100 to 6-MP core provides potential colon targeted system with advantages of reduced gastric exposure and enhanced bioavailability. Formulation can be considered as potential and promising candidate for the treatment of colon diseases..
Keywords: Cancer, colon, compression coating, eudragit RS 100, HPMC K100, 6-Mercaptopurine.
Current Drug Delivery
Title:Optimization of Time Controlled 6-mercaptopurine Delivery for Site- Specific Targeting to Colon Diseases
Volume: 13 Issue: 4
Author(s): Rahul U. Hude and Swati C. Jagdale
Affiliation:
Keywords: Cancer, colon, compression coating, eudragit RS 100, HPMC K100, 6-Mercaptopurine.
Abstract: Background: 6-MP has short elimination time (<2 h) and low bioavailability (~ 50%). Present study was aimed to develop time controlled and site targeted delivery of 6-Mercaptopurine (6-MP) for treatment of colon diseases.
Methods: Compression coating technique was used. 32 full factorial design was designed for optimization of the outer coat for the core tablet. For outer coat amount of Eudragit RS 100 and hydroxypropyl methylcellulose (HPMC K100) were employed as independent variables each at three levels while responses evaluated were swelling index and bursting time. Direct compression method was used for tablets formulation.
Results: 80% w/w of microcrystalline cellulose and 20% w/w of croscarmellose sodium were found to be optimum concentration for the core tablet. The outer coat of optimized batch (ED) contains 21.05% w/w Eudragit RS 100 and 78.95% w/w HPMC K100 of total polymer weight. In-vitro dissolution study indicated that combination of polymer retards the drug release in gastric region and releases ≥95% of drug in colonic region after ≥7 h. Whereas in case of in-vivo placebo x-ray imaging study had shown that the tablet reaches colonic part after 5±0.5 h providing the proof of arrival in the colon. Stability study indicated that the optimized formulation were physically and chemically stable.
Conclusion: Present research work concluded that compression coating by Eudragit RS 100 and HPMC K100 to 6-MP core provides potential colon targeted system with advantages of reduced gastric exposure and enhanced bioavailability. Formulation can be considered as potential and promising candidate for the treatment of colon diseases..
Export Options
About this article
Cite this article as:
U. Hude Rahul and C. Jagdale Swati, Optimization of Time Controlled 6-mercaptopurine Delivery for Site- Specific Targeting to Colon Diseases, Current Drug Delivery 2016; 13 (4) . https://dx.doi.org/10.2174/1567201812666150317123226
DOI https://dx.doi.org/10.2174/1567201812666150317123226 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
Call for Papers in Thematic Issues
Advances of natural products, bio-actives and novel drug delivery system against emerging viral infections
Due to the increasing prevalence of viral infections and the ability of these human pathogens to develop resistance to current treatment strategies, there is a great need to find and develop new compounds to combat them. These molecules must have low toxicity, specific activity and high bioavailability. The most suitable ...read more
Electrospun Fibers as Drug Delivery Systems
In recent years, electrospun fibers have attracted considerable attention as potential platforms for drug delivery due to their distinctive properties and adaptability. These fibers feature a notable surface area-to-volume ratio and can be intentionally designed with high porosity, facilitating an increased capacity for drug loading and rendering them suitable for ...read more
Emerging Nanotherapeutics for Mitigation of Neurodegenerative Disorders
Conditions affecting the central nervous system (CNS) present a significant hurdle due to limited access of both treatments and diagnostic tools for the brain. The blood-brain barrier (BBB) acts as a barrier, restricting the passage of molecules from the bloodstream into the brain. The most formidable challenge facing scientists is ...read more
Nanotechnology Based Chemotherapy for the treatment of Head & Neck Cancer
The escalating recurrence rates observed in Head and Neck cancer, particularly within the chemo-therapeutically treated cohort (50-60%), can be attributed to the non-selective nature of current anticancer drug delivery modalities. In this context, nanotechnology-based drug delivery systems emerge as a promising avenue for achieving precise localization of therapeutic agents to ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Neutrophil-Derived Cytokines: Potential Therapeutic Targets in Inflammation
Current Drug Targets - Inflammation & Allergy <i>Click</i> Reaction in the Synthesis of Dendrimer Drug-delivery Systems
Current Medicinal Chemistry Clinical Implications of COX-1 and / or COX-2 Inhibition for the Distal Gastrointestinal Tract
Current Pharmaceutical Design Antipsoriatic Drug Development: Challenges and New Emerging Therapies
Recent Patents on Inflammation & Allergy Drug Discovery Relevance of Nutritional Antioxidants in Metabolic Syndrome, Ageing and Cancer: Potential for Therapeutic Targeting
Infectious Disorders - Drug Targets Natural compound-derived epigenetic regulators targeting epigenetic readers, writers and erasers
Current Topics in Medicinal Chemistry Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) Induced Dyspepsia
Current Pharmaceutical Design The Discovery and Development of Selective Estrogen Receptor Modulators (SERMs) for Clinical Practice
Current Clinical Pharmacology Efficacy and Safety of Nonopioid Analgesics in Perioperative Pain Control
Current Drug Safety The Regulation of miRNAs in Inflammation-Related Carcinogenesis
Current Pharmaceutical Design Epigenetic Modifications of the Nuclear Factor Kappa B Signalling Pathway and its Impact on Inflammatory Bowel Disease
Current Pharmaceutical Design ADP-Ribosylated Proteins as Old and New Drug Targets for Anticancer Therapy: The Example of ARF6
Current Pharmaceutical Design Potential Role of IL-18 in the Immunopathogenesis of AIDS, HIVAssociated Lipodystrophy and Related Clinical Conditions
Current HIV Research Immunotherapy in Liver Diseases: A Balance Between Immunity and Tolerance
Current Drug Metabolism Appropriate Use of Antibiotics for the Management of Respiratory Tract Infections
Infectious Disorders - Drug Targets Immunomodulatory Properties of Farnesoids: The New Steroids?
Current Medicinal Chemistry Cytochromes P450 in the Bioactivation of Chemicals
Current Topics in Medicinal Chemistry Future Oncotargets: Targeting Overexpressed Conserved Protein Targets in Androgen Independent Prostate Cancer Cell Lines
Anti-Cancer Agents in Medicinal Chemistry 5-HT3 Receptors
Current Drug Targets - CNS & Neurological Disorders An Update on Overcoming MDR1-Mediated Multidrug Resistance in Cancer Chemotherapy
Current Pharmaceutical Design