Nanoencapsulation of water-soluble drug, lamivudine, using a double emulsion spray-drying technique for improving HIV treatment

Tshweu, Lesego; Katata, Lebogang; Kalombo, Lonji; Swai, Hulda

doi:10.1007/s11051-013-2040-4

Cited by 23 publications

(15 citation statements)

References 33 publications

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“…The direction of the magnitude of significance as shown in (5) was negative for ratio of a polymer to a drug indicating an inverse relationship between ratio of a polymer to a drug and EE. This can further be seen from 3D surface plots in Figure 3.…”

Section: Effect Of Independent Variables On Eementioning

confidence: 97%

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Formulation and Optimization of Eudragit RS PO‐Tenofovir Nanocarriers Using Box‐Behnken Experimental Design

Matlhola

Katata-Seru

Tshweu

et al. 2015

Journal of Nanomaterials

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The objective of present study was to develop an optimized polymeric nanoparticle system for the antiretroviral drug tenofovir. A modified nanoprecipitation method was used to prepare Eudragit RS PO nanoparticles of the drug. The effect of amount of polymer, surfactant concentration, and sonication time on particle size, particle distribution, encapsulation efficiency (EE), and zeta potential were assessed and optimized utilizing a three-factor, three-level Box-Behnken Design (BBD) of experiment. Fifteen formulations of nanoparticles were prepared as per BBD and evaluated for particle size, polydispersity index (PDI), EE, and zeta potential. The results showed that the measured mean particle sizes were in the range of 233 to 499 nm, PDI ranged from 0.094 to 0.153, average zeta potential ranged from −19.9 to −45.8 mV, and EE ranged between 98 and 99%. The optimized formulation was characterized for in vitro drug release and structural characterization. The mean particle size of this formulation was 233 nm with a PDI of 0.0107. It had a high EE of 98% and average zeta potential of −35 mV, an indication of particle stability. The FTIR showed some noncovalent interactions between the drug and polymer but a sustained release was observed in vitro for up to 80 hours.

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Section: Effect Of Independent Variables On Eementioning

confidence: 97%

“…Nanoparticles present significant advantages over conventional free drug dosing [5,6]. There is minimal drug loss during transit through the gastrointestinal tract while the particles evade degradation in the acidic environment of the stomach.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Optimization of Eudragit RS PO‐Tenofovir Nanocarriers Using Box‐Behnken Experimental Design

Matlhola

Katata-Seru

Tshweu

et al. 2015

Journal of Nanomaterials

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“…Therefore, some researchers have explored the use of spray-drying as an alternative method to freeze-drying [2,17,[44][45][46].…”

Section: Main Advantages Of the Spray-drying Processmentioning

confidence: 99%

Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers

Sosnik

Seremeta

2015

Advances in Colloid and Interface Science

523

252

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“…A considerable part of investigated systems suffers from the burst release effect, which is usually an unwanted phenomenon limiting their therapeutic suitability. LV-loaded PCL submicron particles were evaluated by Tshweu et al [35]. Drug release from 10 kDa PCL matrices lasted approximately four days, with the initial burst release phase during the first hours of the experiments.…”

Section: Drug Releasementioning

confidence: 99%

Selected Physicochemical and Pharmaceutical Properties of Poly-ε-caprolactone and Poly(d,l-lactide-co-ε-caprolactone) Conjugates of Lamivudine Synthesized via Ring-Opening Polymerization

Urbaniak

Musiał

2019

Polymers

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The modification of drug fate after administration may be achieved by the covalent coupling of active pharmaceutical ingredients with macromolecules. To prolong or delay the release, slowly degrading polymers such as polyesters may be applied for conjugation. The detachment of a covalently conjugated drug from the polymeric matrix relies mostly on the material degradation profile and barely on the weak interaction between the drug and macromolecules. In the present study, lamivudine was conjugated via ring-opening polymerization with poly-ε-caprolactone and poly(d,l-lactide-co-ε-caprolactone). The influence of the reaction parameters on the course of the polymerization and physicochemical properties of obtained conjugates were investigated. Subsequently, selected reaction products were formulated into submicron particles, and drug release profiles in physiological-like conditions were investigated. The course of the reaction was monitored via gel permeation chromatography. The structure and physicochemical properties of products were evaluated via spectroscopic, calorimetric, and diffractometric methods. The profile of the drug release from particles prepared by the slow evaporation of conjugate solution from o/w emulsion was monitored with high-performance liquid chromatography. Both an elevated reaction temperature and higher catalyst concentration increased the polymerization rate and simultaneously promoted the side reactions, resulting in a broad molecular weight distribution of products in the range from 1.30 to 2.15. The physicochemical properties of conjugates obtained in different conditions varied and had a direct influence on the drug release. The release curve of lamivudine from particles based on low molecular weight conjugates achieved a plateau between 18.9 and 22.2 μg per mg of conjugate within a month. Drug detachment from particles composed of high molecular weight conjugates exhibited a distinct delay period preceded by a drug burst release at a maximal level of 13.3 μg per mg of conjugate. Conjugate chemical composition and the degree of crystallinity were also found to influence the release.

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Nanoencapsulation of water-soluble drug, lamivudine, using a double emulsion spray-drying technique for improving HIV treatment

Cited by 23 publications

References 33 publications

Formulation and Optimization of Eudragit RS PO‐Tenofovir Nanocarriers Using Box‐Behnken Experimental Design

Formulation and Optimization of Eudragit RS PO‐Tenofovir Nanocarriers Using Box‐Behnken Experimental Design

Advantages and challenges of the spray-drying technology for the production of pure drug particles and drug-loaded polymeric carriers

Selected Physicochemical and Pharmaceutical Properties of Poly-ε-caprolactone and Poly(d,l-lactide-co-ε-caprolactone) Conjugates of Lamivudine Synthesized via Ring-Opening Polymerization

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