New Insights of Oral Colonic Drug Delivery Systems for Inflammatory Bowel Disease Therapy

Colonic Drug Delivery Systems (CDDS) are especially advantageous for local treatment of inflammatory bowel diseases (IBD). Site-targeted drug release allows to obtain a high drug concentration in injured tissues and less systemic adverse effects, as consequence of less/null drug absorption in small intestine. This review focused on the reported contributions in the last four years to improve the effectiveness of treatments of inflammatory bowel diseases. The work concludes that there has been an increase in the development of CDDS in which pH, specific enzymes, reactive oxygen species (ROS), or a combination of all of these triggers the release. These delivery systems demonstrated a therapeutic improvement with fewer adverse effects. Future perspectives to the treatment of this disease include the elucidation of molecular basis of IBD diseases in order to design more specific treatments, and the performance of more in vivo assays to validate the specificity and stability of the obtained systems.

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Guar gum-based colon-specific drug delivery systems for the treatment of Inflammatory Bowel Diseases

Inflammatory Bowel Diseases ◽

10.1097/00054725-200912002-00175 ◽

2009 ◽

Vol 15 ◽

pp. S56

Author(s):

S Yellela ◽

S S ◽

R YV

Keyword(s):

Drug Delivery ◽

Inflammatory Bowel Diseases ◽

Drug Delivery Systems ◽

Guar Gum ◽

Delivery Systems ◽

Specific Drug ◽

Bowel Diseases ◽

Inflammatory Bowel ◽

Colon Specific Drug Delivery

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Oral colon targeted delivery systems for treatment of inflammatory bowel diseases: Synthesis, in vitro and in vivo assessment

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2008.04.021 ◽

2008 ◽

Vol 358 (1-2) ◽

pp. 248-255 ◽

Cited By ~ 30

Author(s):

Amal H. El-Kamel ◽

Alaa A.-M. Abdel-Aziz ◽

Amal J. Fatani ◽

Hussein I. El-Subbagh

Keyword(s):

Inflammatory Bowel Diseases ◽

Targeted Delivery ◽

Delivery Systems ◽

Bowel Diseases ◽

Inflammatory Bowel ◽

In Vivo Assessment ◽

Targeted Delivery Systems

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Strategic Approaches for Colon Targeted Drug Delivery: An Overview of Recent Advancements

Pharmaceutics ◽

10.3390/pharmaceutics12010068 ◽

2020 ◽

Vol 12 (1) ◽

pp. 68 ◽

Cited By ~ 18

Author(s):

Sang Hoon Lee ◽

Rajiv Bajracharya ◽

Jeong Youn Min ◽

Ji-Won Han ◽

Byeong Ju Park ◽

...

Keyword(s):

Drug Delivery ◽

Targeted Drug Delivery ◽

Oral Delivery ◽

Drug Delivery Systems ◽

Local Treatment ◽

Delivery Systems ◽

Therapeutic Benefits ◽

Colonic Drug Delivery ◽

Targeted Drug ◽

Targeted Drug Delivery Systems

Colon targeted drug delivery systems have gained a great deal of attention as potential carriers for the local treatment of colonic diseases with reduced systemic side effects and also for the enhanced oral delivery of various therapeutics vulnerable to acidic and enzymatic degradation in the upper gastrointestinal tract. In recent years, the global pharmaceutical market for biologics has grown, and increasing demand for a more patient-friendly drug administration system highlights the importance of colonic drug delivery as a noninvasive delivery approach for macromolecules. Colon-targeted drug delivery systems for macromolecules can provide therapeutic benefits including better patient compliance (because they are pain-free and can be self-administered) and lower costs. Therefore, to achieve more efficient colonic drug delivery for local or systemic drug effects, various strategies have been explored including pH-dependent systems, enzyme-triggered systems, receptor-mediated systems, and magnetically-driven systems. In this review, recent advancements in various approaches for designing colon targeted drug delivery systems and their pharmaceutical applications are covered with a particular emphasis on formulation technologies.

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Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v6i1.8883 ◽

2016 ◽

Vol 6 (1) ◽

Author(s):

Anamika Saxena Saxena ◽

Santosh Kitawat ◽

Kalpesh Gaur ◽

Virendra Singh

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery Systems ◽

Entrapment Efficiency ◽

Repeated Administration ◽

Alginate Beads ◽

Delivery Systems ◽

Sem Analysis ◽

Formulation Development

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.

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Nanostructured Ketorolac-Tromethamine/MCF: Synthesis, Characterization and Application in Drug Release System

Current Nanoscience ◽

10.2174/1573413714666180222134742 ◽

2018 ◽

Vol 14 (5) ◽

pp. 432-439 ◽

Cited By ~ 1

Author(s):

Juliana M. Juarez ◽

Jorgelina Cussa ◽

Marcos B. Gomez Costa ◽

Oscar A. Anunziata

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Therapeutic Efficacy ◽

Drug Delivery Systems ◽

Controlled Drug Release ◽

Delivery Systems ◽

The Body ◽

Fickian Diffusion ◽

Ketorolac Tromethamine

Background: Controlled drug delivery systems can maintain the concentration of drugs in the exact sites of the body within the optimum range and below the toxicity threshold, improving therapeutic efficacy and reducing toxicity. Mesostructured Cellular Foam (MCF) material is a new promising host for drug delivery systems due to high biocompatibility, in vivo biodegradability and low toxicity. Methods: Ketorolac-Tromethamine/MCF composite was synthesized. The material synthesis and loading of ketorolac-tromethamine into MCF pores were successful as shown by XRD, FTIR, TGA, TEM and textural analyses. Results: We obtained promising results for controlled drug release using the novel MCF material. The application of these materials in KETO release is innovative, achieving an initial high release rate and then maintaining a constant rate at high times. This allows keeping drug concentration within the range of therapeutic efficacy, being highly applicable for the treatment of diseases that need a rapid response. The release of KETO/MCF was compared with other containers of KETO (KETO/SBA-15) and commercial tablets. Conclusion: The best model to fit experimental data was Ritger-Peppas equation. Other models used in this work could not properly explain the controlled drug release of this material. The predominant release of KETO from MCF was non-Fickian diffusion.

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Anti-TNF-α Treatment Reduces the Baseline Procoagulant Imbalance of Patients With Inflammatory Bowel Diseases

Inflammatory Bowel Diseases ◽

10.1093/ibd/izaa351 ◽

2021 ◽

Author(s):

Armando Tripodi ◽

Luisa Spina ◽

Laura Francesca Pisani ◽

Lidia Padovan ◽

Flaminia Cavallaro ◽

...

Keyword(s):

Inflammatory Bowel Diseases ◽

Coagulation Factors ◽

Infliximab Treatment ◽

C Reactive Protein ◽

Reactive Protein ◽

Thrombosis Risk ◽

Bowel Diseases ◽

Inflammatory Bowel ◽

Factor Α

Abstract Background Inflammatory bowel diseases (IBD) are characterized by an increased thrombosis risk of uncertain etiology. Coagulation derangement arising from inflammation may be a triggering factor. We hypothesized that strong inflammation inhibitors (eg, anti-tumor necrosis factor-α drugs) may affect coagulation. Methods Forty patients with IBD were compared with 57 control patients for coagulation factors and endogenous thrombin potential (ETP), the latter being the most sensitive marker of in vivo pro- and anticoagulation balance. We measured ETP in the presence and absence of thrombomodulin (the physiologic protein C [PC] activator). Coagulation at different timepoints was also assessed for 28 of these patients during infliximab treatment. Results The median ETP (nM thrombin × minutes) and range (minimum-maximum) were each higher in patients at baseline than in control patients in both the absence (2120 [1611-3041] vs 1865 [1270-2337]) and the presence (1453 [464-2522] vs 831 [104-1741]) of thrombomodulin. The ETP ratio (with/without thrombomodulin) was high at baseline (0.73 [0.21-0.90] vs 0.45 [0.07-0.85]). The ETP and ETP ratio declined during treatment and were significantly lower at the end than at baseline. Factor (F) VIII and fibrinogen, which were high at baseline, decreased during treatment and at the end were significantly lower than at baseline. The FVIII/PC ratio, which was high in patients at baseline, declined during treatment and at the end was lower than at baseline. C-reactive protein recorded at the end of treatment was lower than at baseline. Conclusions Patients with IBD have a procoagulant imbalance as shown by increased ETP at baseline. The ETP decreases during treatment with infliximab, which is related to decreased FVIII and FVIII/PC ratio. This effect is also related to the improvement of inflammation as shown by decreased fibrinogen and C-reactive protein.

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Mechanisms and Pharmaceutical Action of Lipid Nanoformulation of Natural Bioactive Compounds as Efficient Delivery Systems in the Therapy of Osteoarthritis

Pharmaceutics ◽

10.3390/pharmaceutics13081108 ◽

2021 ◽

Vol 13 (8) ◽

pp. 1108

Author(s):

Oana Craciunescu ◽

Madalina Icriverzi ◽

Paula Ecaterina Florian ◽

Anca Roseanu ◽

Mihaela Trif

Keyword(s):

Drug Delivery ◽

Bioactive Compounds ◽

Targeted Delivery ◽

Drug Delivery Systems ◽

Delivery Systems ◽

Joint Disease ◽

Duration Of Action ◽

Immune System Activation

Osteoarthritis (OA) is a degenerative joint disease. An objective of the nanomedicine and drug delivery systems field is to design suitable pharmaceutical nanocarriers with controllable properties for drug delivery and site-specific targeting, in order to achieve greater efficacy and minimal toxicity, compared to the conventional drugs. The aim of this review is to present recent data on natural bioactive compounds with anti-inflammatory properties and efficacy in the treatment of OA, their formulation in lipid nanostructured carriers, mainly liposomes, as controlled release systems and the possibility to be intra-articularly (IA) administered. The literature regarding glycosaminoglycans, proteins, polyphenols and their ability to modify the cell response and mechanisms of action in different models of inflammation are reviewed. The advantages and limits of using lipid nanoformulations as drug delivery systems in OA treatment and the suitable route of administration are also discussed. Liposomes containing glycosaminoglycans presented good biocompatibility, lack of immune system activation, targeted delivery of bioactive compounds to the site of action, protection and efficiency of the encapsulated material, and prolonged duration of action, being highly recommended as controlled delivery systems in OA therapy through IA administration. Lipid nanoformulations of polyphenols were tested both in vivo and in vitro models that mimic OA conditions after IA or other routes of administration, recommending their clinical application.

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