Development of a multiple unit drug delivery system for positioned release in the gastrointestinal tract

1991 ◽  
Vol 15 (2) ◽  
pp. 105-112 ◽  
Author(s):  
K. Klokkers-Bethke ◽  
W. Fischer
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Drug Delivery System ◽  
Delivery System ◽  
Multiple Unit

A Conceptual Analysis of solid Self-emulsifying drug Delivery System and its Associate Patents for the Treatment of Cancer

2020 ◽  
Vol 14 ◽  
Author(s):  
Neeraj Singh ◽  
Shweta Rai ◽  
Sankha Bhattacharya
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Review Article ◽  
New Drugs ◽  
Systemic Absorption ◽  
Hydrophobic Drugs ◽  
Drug Bioavailability

Background: About two-third of new drugs reveal low solubility in water due to that; it becomes difficult for formulation scientists to develop oral solid dosage forms with a pharmaceutically acceptable range of therapeutic activity. In such cases, S-SMEEDS are the best carrier used universally for the delivery of hydrophobic drugs. SEDDS were also used, but due to its limitations, S-SMEDDS used widely. These are the isotropic mixtures of oils, co-solvents, and surfactants. S-SMEDDS are physically stable, easy to manufacture, easy to fill in gelatin capsules as well as improves the drug bioavailability by releasing the drug in the emulsion form to the gastrointestinal tract and make smooth absorption of the drug through the intestinal lymphatic pathway. Methods: We took on the various literature search related to our review, including the peer-reviewed research, and provided a conceptual framework to that. Standard tools are used for making the figures of the paper, and various search engines are used for the literature exploration.In this review article the author discussed the importance of S-SMEDDS, selection criteria for excipients, pseudo-ternary diagram, mechanism of action of S-SMEDDS, solidification techniques used for S-SMEDDS, Characterization of SEDDS and S-SMEDDS including Stability Evaluation of both and future prospect concluded through recent findings on S-SMEDDS on Cancer as well as a neoteric patent on S-SMEDDS Results: Many research papers discussed in this review article, from which it was found that the ternary phase diagram is the most crucial part of developing the SMEDDS. From the various research findings, it was found that the excipient selection is the essential step which decides the strong therapeutic effect of the formulation. The significant outcome related to solid-SMEDDS is less the globule size, higher would be the bioavailability. The adsorption of a solid carrier method is the most widely used method for the preparation of solid-SMEDDS. After review of many patents, it is observed that the solid-SMEDDS have a strong potential for targeting and treatment of a different type of Cancer due to their property to enhance permeation and increased bioavailability. Conclusion: S-SMEEDS are more acceptable pharmaceutically as compare to SEDDS due to various advantages over SEDDS viz stability issue is prevalent with SEDDS. A number of researchers had formulated S-SMEDDS of poorly soluble drugs and founded S-SMEDDS as prospective for the delivery of hydrophobic drugs for the treatment of Cancer. S-SMEEDS are grabbing attention, and the patentability on S-SMEDDS is unavoidable, these prove that S-SMEEDS are widely accepted carriers. These are used universally for the delivery of the hydrophilic drugs and anticancer drugs as it releases the drug to the gastrointestinal tract and enhances the systemic absorption. Abstract: Majority of active pharmaceutical ingredients (API) shows poor aqueous solubility, due to that drug delivery of the API to the systemic circulation becomes difficult as it has low bioavailability. The bioavailability of the hydrophobic drugs can be improved by the Self-emulsifying drug delivery system (SEDDS) but due to its various limitations, solid self-micro emulsifying drug delivery systems (S-SMEDDS) are used due to its advantages over SEDDS. S-SMEDDS plays a vital role in improving the low bioavailability of poorly aqueous soluble drugs. Hydrophobic drugs can be easily loaded in these systems and release the drug to the gastrointestinal tract in the form of fine emulsion results to In-situ solubilisation of the drug. In this review article the author's gives an overview of the solid SMEDSS along with the solidification techniques and an update on recent research and patents filled for Solid SMEDDS.

Dissolution and Pharmacokinetic Properties of Alkaloids and Flavonoids in a Xiexin Multiple-unit Drug Delivery System

Drug Research ◽  
2013 ◽  
Vol 63 (10) ◽  
pp. 501-509 ◽  
Author(s):  
Y. Xie ◽  
Y. Hu ◽  
M. Shen ◽  
Y. Ma ◽  
J. Zhong ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Pharmacokinetic Properties ◽  
Multiple Unit

scholarly journals Development of a novel drug delivery system to deliver drugs directly to the colonic mucosa, resulting in improved efficacy and reduced systemic exposure for the treatment of ulcerative colitis

2021 ◽  
Author(s):  
Merodean Huntsman ◽  
Shaoying N Lee ◽  
Jack Stylli ◽  
Cheryl Stork ◽  
Jeff Shimizu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Exposure ◽  
New Technologies ◽  
Systemic Exposure ◽  
Physiological Variables ◽  
Novel Drug Delivery System ◽  
Novel Drug

Abstract Despite recent drug approvals for the treatment of inflammatory bowel diseases (IBD), there remains a high unmet need for new technologies that can increase drug efficacy by improving site-specific drug delivery while reducing systemic exposure. These technologies must address challenges with formulation; in particular, drugs that are liquid, peptides or proteins are difficult to formulate using existing delayed and extended oral release technologies. They also have the potential to improve efficacy and reduce systemic exposure for certain drugs by delivering higher doses directly to the site of inflammation. A novel drug delivery system (DDS2) is being developed for delivery at a pre-specified part of the gastrointestinal tract. This autonomous mechanical capsule uses an algorithm based on reflected light to deliver soluble formulations of drugs to the predefined location. This system has significant advantages over other traditional delayed release oral formulations because it functions independently of human physiological variables such as pH and transit time and can deliver liquid formulations, peptides, and proteins. Such a system can ensure a predictable high luminal drug exposure and limited degradation or systemic absorption in the upper gastrointestinal tract and would therefore be ideal for treatment of disorders such as IBD and colon cancer.

scholarly journals Improved Safety and Anti-Glioblastoma Efficacy of CAT3-Encapsulated SMEDDS through Metabolism Modification

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 484
Author(s):  
Hongliang Wang ◽  
Lin Li ◽  
Jun Ye ◽  
Wujun Dong ◽  
Xing Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Side Effects ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lymphatic Transport ◽  
Pharmacokinetic Parameters ◽  
Gastrointestinal Side Effects ◽  
The Brain

13a-(S)-3-pivaloyloxyl-6,7-dimethoxyphenanthro(9,10-b)-indolizidine (CAT3) is a novel oral anti-glioma pro-drug with a potent anti-tumor effect against temozolomide-resistant glioma. 13a(S)-3-hydroxyl-6,7-dimethoxyphenanthro(9,10-b)-indolizidine (PF403) is the active in vivo lipase degradation metabolite of CAT3. Both CAT3 and PF403 can penetrate the blood–brain barrier to cause an anti-glioma effect. However, PF403, which is produced in the gastrointestinal tract and plasma, causes significant gastrointestinal side effects, limiting the clinical application of CAT3. The objective of this paper was to propose a metabolism modification for CAT3 using a self-microemulsifying drug delivery system (SMEDDS), in order to reduce the generation of PF403 in the gastrointestinal tract and plasma, as well as increase the bioavailability of CAT3 in vivo and the amount of anti-tumor substances in the brain. Thus, a CAT3-loaded self-microemulsifying drug delivery system (CAT3-SMEDDS) was prepared, and its physicochemical characterization was systematically carried out. Next, the pharmacokinetic parameters of CAT3 and its metabolite in the rats’ plasma and brain were measured. Furthermore, the in vivo anti-glioma effects and safety of CAT3-SMEDDS were evaluated. Finally, Caco-2 cell uptake, MDCK monolayer cellular transfer, and the intestinal lymphatic transport mechanisms of SMEDDS were investigated in vitro and in vivo. Results show that CAT3-SMEDDS was able to form nanoemulsion droplets in artificial gastrointestinal fluid within 1 min, displaying an ideal particle size (15–30 nm), positive charge (5–9 mV), and controlled release behavior. CAT3-SMEDDS increased the membrane permeability of CAT3 by 3.9-fold and promoted intestinal lymphatic transport. Hence, the bioavailability of CAT3 was increased 79% and the level of its metabolite, PF403, was decreased to 49%. Moreover, the concentrations of CAT3 and PF403 were increased 2–6-fold and 1.3–7.2-fold, respectively, in the brain. Therefore, the anti-glioma effect in the orthotopic models was improved with CAT3-SMEDDS compared with CAT3 in 21 days. Additionally, CAT3-SMEDDS reduced the gastrointestinal side effects of CAT3, such as severe diarrhea, necrosis, and edema, and observed less inflammatory cell infiltration in the gastrointestinal tract, compared with the bare CAT3. Our work reveals that, through the metabolism modification effect, SMEDDS can improve the bioavailability of CAT3 and reduce the generation of PF403 in the gastrointestinal tract and plasma. Therefore, it has the potential to increase the anti-glioma effect and reduce the gastrointestinal side effects of CAT3 simultaneously.

scholarly journals Preparation andIn VitroRelease of Drug-Loaded Microparticles for Oral Delivery Using Wholegrain Sorghum Kafirin Protein

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Esther T. L. Lau ◽  
Stuart K. Johnson ◽  
Roger A. Stanley ◽  
Deirdre Mikkelsen ◽  
Zhongxiang Fang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Drug Delivery System ◽  
Delivery System ◽  
Targeted Delivery ◽  
Oral Delivery ◽  
Protein Digestibility ◽  
Target Area ◽  
Sorghum Grains

Kafirin microparticles have been proposed as an oral nutraceutical and drug delivery system. This study investigates microparticles formed with kafirin extracted from white and raw versus cooked red sorghum grains as an oral delivery system. Targeted delivery to the colon would be beneficial for medication such as prednisolone, which is used in the management of inflammatory bowel disease. Therefore, prednisolone was loaded into microparticles of kafirin from the different sources using phase separation. Differences were observed in the protein content,in vitroprotein digestibility, and protein electrophoretic profile of the various sources of sorghum grains, kafirin extracts, and kafirin microparticles. For all of the formulations, the majority of the loaded prednisolone was not released inin vitroconditions simulating the upper gastrointestinal tract, indicating that most of the encapsulated drug could reach the target area of the lower gastrointestinal tract. This suggests that these kafirin microparticles may have potential as a colon-targeted nutraceutical and drug delivery system.

Suitable Polymers in Floating Gastro-Retentive Drug Delivery

2020 ◽  
pp. 371-382
Author(s):  
Kaustubh Gavali ◽  
Preeti Karade
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Targeted Delivery ◽  
Floating Drug Delivery ◽  
Effect Of Food ◽  
Multiple Unit ◽  
Novel Drug ◽  
Absorption Window ◽  
Gastro Retentive

Gastro-retentive drug delivery is novel drug delivery system which is emerged for controlled and targeted delivery of drug especially when target site lies in or near the stomach. The drug with absorption window in stomach, locally acting drug in stomach, etc. are the best suitable candidate for this drug delivery system. It can be formulated in various types like floating, expandable & unfoldable, Raft forming, swelling system Bio adhesive, High density system etc. The gastro-retentive form can be used in various dosage forms like tablet, capsule, microsphere, granules, powders, pills and laminated films according to the need. It can be also formulated as single unit and multiple unit dosage form but sometime this gastro-retention is unpredictable due to effect of pH, gastric mobility, effect of food etc. This review mainly focuses on the floating drug delivery its types, polymer used in floating drug delivery and application.

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