Formulation and Optimization of Artemether And Lumefantrine Calcium Alginate Capsules Using Inverse Gelation Technique

Filed in Articles by on July 6, 2022

Formulation and Optimization of Artemether And Lumefantrine Calcium Alginate Capsules Using Inverse Gelation Technique.

ABSTRACT  

Poorly water-soluble drug candidates are associated with dissolution, absorption and bioavailability challenges. Consequently, poor solubility and non-reproducible absorption from the gastrointestinal tract following oral administration constitute a biopharmaceutical concern to dosage form design and formulation.

The use of lipid-based formulations to address this concern has been the choice of many scientists in the drug delivery domain.

Artemether and Lumefantrine the drugs investigated in the work are poorly soluble with unpredictable absorption and bioavailability problems. In addition, they may be prone to acid hydrolysis and precipitation respectively in gastric environment of the stomach.

To date there is no published work on alginate capsules geared towards solving bioavailability problems and inactivation of Artemether and Lumefantrine in the stomach.

In this work we aimed at employing optimized lipid-based formulation capable of solubilizing artemether and lumefantrine, and protecting artemether from possible stomach acid degradation using alginate capsules, for ultimate avoidance of resistance and improved antimalarial performance.

A 33 full factorial experimental design was employed to optimize excipient compositions using JMP Discovery V10 Statistical Software. 

LITERATURE EVALUATION  

Drug delivery refers to different ways of administering drugs to the body needed to safely achieve its desired therapeutic effect. It involves targeting a drug to a particular site within the body. Drug delivery is often approached via a drug’s chemical formulation, but it may also involve medical devices or drug-device combination products.

Drug delivery is a concept heavily integrated with dosage form and route of administration, the latter sometimes even being considered part of the definition.

Drug delivery technologies modify drug release profile, absorption, distribution and elimination for the benefit of improving product efficacy and safety, as well as patient convenience and compliance. Drug release is from: diffusion, degradation, swelling, and affinity-based mechanisms. 

Most common routes of administration include the preferred non-invasive peroral (through the mouth), topical (skin), transmucosal (nasal, buccal/sublingual, vaginal, ocular and rectal) and inhalation routes.

Current efforts in the area of drug delivery include the development of targeted delivery in which the drug is only active in the target area of the body (for example, in cancerous tissues),

sustained release formulations in which the drug is released over a period of time in a controlled manner from a formulation, and methods to increase survival of peroral agents which must pass through the stomach’s acidic environment. 

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CSN Team.

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