Formulation and Characterisation of Sustained Release Microbeads Loaded With Zaltoprofen

Kiran, Habiba; Dhandapani, Nagasamy Venkatesh; Raman, R.

doi:10.22159/ijap.2019v11i5.34750

Cited by 6 publications

(4 citation statements)

References 8 publications

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“…For example, an ibuprofen derivative, zaltoprofen, used to treat acute pains [110], is a non-ionic compound that cannot form salts. As an NSAID, this drug is poorly soluble and has been formulated as a sustained-release dosage form [111], mixed with a surfactant to increase the solubility [112]. However, this neutral compound can still be combined with nicotinamide via the non-ionic reaction to form a multi-component solid, which has been proven to improve its physicochemical properties [113].…”

Section: Fluoroquinolone-nsaid Multi-componentsmentioning

confidence: 99%

The Benefits and Challenges of Antibiotics–Non-Steroidal Anti-Inflammatory Drugs Non-Covalent Reaction

2023

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Recently, non-covalent reactions have emerged as approaches to improve the physicochemical properties of active pharmaceutical ingredients (API), including antibiotics and non-steroidal anti-inflammatory drugs (NSAIDs). This review aimed to present and discuss the non-covalent reaction products of antibiotics, including salt and neutral multi-component solid forms, by framing their substituents and molar ratios, manufacturing techniques, characterization methods, benefits, potency changes, and toxicity, and is completed with an analysis of the development of computational models used in this field. Based on the data, NSAIDs are the most-developed drugs in multi-component system preparations, followed by antibiotics, i.e., antituberculosis and fluoroquinolones. They have reacted with inorganic elements, excipients, nutraceuticals, natural products, and other drugs. However, in terms of treatments for common infections, fluoroquinolones are more frequently used. Generally, NSAIDs are acquired on an over-the-counter basis, causing inappropriate medication. In addition, the pKa differences between the two groups of medicine offer the potential for them to react non-covalently. Hence, this review highlights fluoroquinolone–NSAID multi-component solid systems, which offer some benefits. These systems can increase patient compliance and promote the appropriate monitoring of drug usage; the dual drug multi-component solids have been proven to improve the physicochemical properties of one or both components, especially in terms of solubility and stability. In addition, some reports show an enhancement of the antibiotic activity of the products. However, it is important to consider the possibility of activity changes, interaction, and toxicity when using drug combinations. Hence, these aspects also are discussed in this review. Finally, we present computational modeling, which has been utilized broadly to support multi-component system designs, including coformer screening, preparation methods, and structural modeling, as well as to predict physicochemical properties, potency, and toxicity. This integrated review is expected to be useful for further antibiotic–NSAID multi-component system development.

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Section: Fluoroquinolone-nsaid Multi-componentsmentioning

confidence: 99%

The Benefits and Challenges of Antibiotics–Non-Steroidal Anti-Inflammatory Drugs Non-Covalent Reaction

2023

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“…The microspheres of OX were prepared by ionotropic gelation technique [24][25][26]. OX (0.25% w/v) was added to an aqueous solution of sodium alginate and stirred thoroughly for 15 min.…”

Section: Preparation Of Oxaliplatin Microspheresmentioning

confidence: 99%

DEVELOPMENT OF pH-DEPENDENT CHRONOMODULATED DELIVERY SYSTEMS OF 5-FLUOROURACIL AND OXALIPLATIN TO TREAT COLON CANCER

et al. 2020

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Objective: To develop two different oral formulations such as 5-fluorouracil (5-FU) tablets and oxaliplatin (OX) microspheres which were further filled into capsules and coated with pH-sensitive polymer (eudragit S-100) for the chronotherapeutic treatment of colon cancer (Fluorouracil: Oxaliplatin regimen) to perform as a substitute for intravenous (IV) route based chronomodulated chemotherapy. Methods: The 5-FU tablet formulation was prepared with alginate and guar gum polymers in varied concentrations using wet granulation technique in two varieties such as granules coated and tablet coated formulations using eudragit RSPO as coating material to achieve controlled drug release. Alongside OX microspheres were formulated using the ionotropic gelation methodology in combination with alginate and chitosan polymers in varying concentrations to accomplish a time-controlled drug release. Prepared formulations were evaluated for pre-compression and post-compression parameters, percentage yield, percentage drug entrapment, Fourier transformed infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC), Scanning electron microscopy (SEM), In vitro and Ex vivo dissolution studies. Results: Pre-compression and post-compression parameters for 5-FU tablets were satisfied with Indian pharmacopeia specifications. The entrapment efficiency of OX microspheres were increased due to the elevated concentration of polymers up to a certain level as seen in A7M, further greater the concentration of polymer resulted in a decline of entrapment efficiency as seen in A4M and A8M. The optimized formulations A14T and A14M were shown in vitro drug release of 90.36 % by 24 h and 79.63 % by 9 h respectively. Conclusion: The two different oral formulations of 5-FU (Tablets) and OX (Microspheres) were found to be successful in controlled drug release. Therefore they can be efficiently used to control the rate of drug release to the colon in synchronization with the circadian timing system in the belief of improved therapeutic efficacy, tolerability and overall survival rate of cancer patients. Hence it is promised to be a better alternative for intravenous route based chronomodulated chemotherapy.

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“…Our lakes, rivers, and ocean are filled with these little particles that wastewater treatment systems are unable to filter out. What's worse is that these microplastics may act as microscopic chemical and toxin transfer stations [4] .…”

Section: Introductionmentioning

confidence: 99%

A review on micro beads: Formulation, technological aspects, and extraction

Shaik Khaja Moinuddin,

Pradeep Kumar M,

Sandeep Kumar G

et al. 2024

GSC Biol. Pharm. Sci.

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Any drug delivery system's purpose is to deliver a therapeutic amount of medicine to the appropriate place in the body while also achieving and maintaining the correct drug concentration. This could be accomplished by using numerous unit dosage forms such as microgranules/spheroids, pellets, microcapsules, and beads, which are divided into many separate units, referred to as subunits, each of which possesses certain desired features. The advantages of micro particle drug delivery systems over single unit dose form are well documented. One of the solutions that does not entail the use of harsh chemicals or elevated temperatures is the production of microbeads medication delivery systems. The traditional procedures require the use of ionotropic gelation methods, which include internal and external gelation methods, emulsion gelation methods, polyelectrolyte complexation methods, and so on. Because of the ease of preparation, the majority of work has been done on the preparation of microbeads using the ionotropic gelation process rather than alternative approaches.

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Formulation and Characterisation of Sustained Release Microbeads Loaded With Zaltoprofen

Cited by 6 publications

References 8 publications

The Benefits and Challenges of Antibiotics–Non-Steroidal Anti-Inflammatory Drugs Non-Covalent Reaction

The Benefits and Challenges of Antibiotics–Non-Steroidal Anti-Inflammatory Drugs Non-Covalent Reaction

DEVELOPMENT OF pH-DEPENDENT CHRONOMODULATED DELIVERY SYSTEMS OF 5-FLUOROURACIL AND OXALIPLATIN TO TREAT COLON CANCER

A review on micro beads: Formulation, technological aspects, and extraction

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