Sustained-release liquisolid compact tablets containing artemether-lumefantrine as alternate-day regimen for malaria treatment to improve patient compliance

Nnamani, Petra O.; Ugwu, Agatha; Ibezim, EC; Kenechukwu, Franklin Chimaobi; Akpa, Paul A.; Ogbonna, John-Dike N.; Obitte, Nicholas C.; Odo, Amelia Ngozi; Windbergs, Maike; Lehr, Claus‐Michael; Attama, Anthony A.

doi:10.2147/ijn.s92755

Cited by 13 publications

(14 citation statements)

References 30 publications

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“…Liquisolid compact tablets or capsules can be obtained after lipid dispersions are loaded into adsorptive excipients and form dry-looking, freely flowing and compressible powders. For example, Nnamani et al developed low-dose liquisolid tablets of artemether-lumefantrine (AL) from NLCs and estimated their potential for oral delivery of AL in malariogenic Wistar mice [ 192 ]. The results highlighted that AL-loaded NLCs could be further processed into oral tablets to improve the patient’s compliance.…”

Section: Lipid Dispersion Techniquementioning

confidence: 99%

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

et al. 2018

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Over the past decades, a large number of drugs as well as drug candidates with poor dissolution characteristics have been witnessed, which invokes great interest in enabling formulation of these active ingredients. Poorly water-soluble drugs, especially biopharmaceutical classification system (BCS) II ones, are preferably designed as oral dosage forms if the dissolution limit can be broken through. Minimizing a drug’s size is an effective means to increase its dissolution and hence the bioavailability, which can be achieved by specialized dispersion techniques. This article reviews the most commonly used dispersion techniques for pharmaceutical processing that can practically enhance the dissolution and bioavailability of poorly water-soluble drugs. Major interests focus on solid dispersion, lipid-based dispersion (nanoencapsulation), and liquisolid dispersion (drug solubilized in a non-volatile solvent and dispersed in suitable solid excipients for tableting or capsulizing), covering the formulation development, preparative technique and potential applications for oral drug delivery. Otherwise, some other techniques that can increase the dispersibility of a drug such as co-precipitation, concomitant crystallization and inclusion complexation are also discussed. Various dispersion techniques provide a productive platform for addressing the formulation challenge of poorly water-soluble drugs. Solid dispersion and liquisolid dispersion are most likely to be successful in developing oral dosage forms. Lipid-based dispersion represents a promising approach to surmounting the bioavailability of low-permeable drugs, though the technique needs to traverse the obstacle from liquid to solid transformation. Novel dispersion techniques are highly encouraged to develop for formulation of poorly water-soluble drugs.

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Section: Lipid Dispersion Techniquementioning

confidence: 99%

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

et al. 2018

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“…Accurately weighed 100 mg of drug film (CARART and/or PROART) was transferred to a 100 ml volumetric flask and dissolved with 5 ml of ethanol. To it, 25 ml of 1N HCl was added and heated using thermo-regulated water bath for 30 min at temperature of 80±2 o C, slightly modified according to an earlier method 37 . The solution was allowed to cool at room temperature, filtered and the volume was made up to 100 ml mark with deionized water and/or simulated salivary fluid, SSF (pH 6.5).…”

Section: Drug Content Analysismentioning

confidence: 99%

“…Different release models 37 were applied to study the kinetics and mechanisms of ART release from mucoadhesive films including zero order, first order, Higuchi and Korsmeyer-Peppas models. First order assessed log cumulative of % drug remaining versus time whereas zero order was done by fitting cumulative % drug release versus time 38 .…”

Section: Dissolution Rate Studies and Drug Release Kineticsmentioning

confidence: 99%

“…Evaluation of the curative effect of formulated films against established plasmodium infection was carried out 37 . On the day 0 of the test, percentage parasitemia and red blood cell count of the donor mice was determined by a Giemsa-stained thin blood smear of the donor mice and improved Neubauer counting chamber respectively.…”

Section: 15mentioning

confidence: 99%

“…Other prominent points of interaction were at 1900 cm -1 between CARART and ART due to aromaticity. PROART and ART had more prominent points of interaction at 2400, 1650-1590 (primary amine NH bend from PRO) and 1680-1620 cm -1 due to aromaticity (C=C) 37 .…”

Section: Infrared (Ftir) Analysismentioning

confidence: 99%

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In vivo antiplasmodial potential of Carrageenan and Prosopis africana buccal films of artemether on malariogenic mice

Nnamani

Nnadi

Ibezim

et al. 2020

J. Drug Delivery Ther.

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Objective: To deliver bioadhesive buccal films of artemether (ART) with ability to adhere, hydrate and release drug across the buccal membrane. Methods: Buccal films prepared by film casting using carrageenan (CAR) and Prosopis africana (PRO) were characterized by size, zeta potential, texture, water content, morphology, thermal and interaction studies, in vitro and in vivo antiplasmodial activity in mice. Results: Films were stable with sizes (2442 and 835 nm), water content (21 and 15 %), bioadhesivity (24 and 9.4 %) and film thickness (0.18 and 0.28 mm) for CARART and PROART respectively. Enthalpy of CARART, PROART and ART were 76, 22 and 88 J/g where as parasitaemia reduction of 67 and 76 % were observed for CARART and PROART respectively. Conclusion: Though CARART had better water content and bioadhesivity necessary for film hydration at buccal membrane, PROART eventually had superior buccal performance perhaps due to its film thickness and amorphous nanoparticle subdivision. Key words: Artemether; Carrageenan; Prosopis africana; Sublingual buccal films; Malaria

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Liquisolid Technique: a Novel Tool to Develop Aceclofenac-Loaded Eudragit L-100 and RS-100-Based Sustained Release Tablets

Hussain

Shah

2020

J Pharm Innov

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Sustained-release liquisolid compact tablets containing artemether-lumefantrine as alternate-day regimen for malaria treatment to improve patient compliance

Cited by 13 publications

References 30 publications

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

In vivo antiplasmodial potential of Carrageenan and Prosopis africana buccal films of artemether on malariogenic mice

Liquisolid Technique: a Novel Tool to Develop Aceclofenac-Loaded Eudragit L-100 and RS-100-Based Sustained Release Tablets

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