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1.
Polim Med ; 52(2): 83-92, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36268746

RESUMO

BACKGROUND: Mucilage and pectin are both natural polymers with the advantages of availability and biodegradability. Microspheres made from biodegradable polymers can break down naturally after performing their tasks. OBJECTIVES: The study aimed to use mucilage and pectin from the leaves of Talinum triangulare (Jacq.) Willd. as polymer matrices for the formulation of microspheres, with ibuprofen as the model drug. MATERIAL AND METHODS: Both polymers were examined under a microscope and evaluated using measurements of viscosity, density, flow properties, swelling power, elemental analysis, Fourier-transform infrared spectroscopy (FTIR), and the degree of esterification (DE) for pectin. The microspheres were prepared using the ionotropic gelation method and alginate:mucilage/pectin at ratios of 1:1 and 1:2. They were assessed for swellability, drug entrapment effectiveness and drug release profile. RESULTS: The mucilage particles were ovoid while pectin particles were irregularly shaped. Pectin had higher particle, bulk and tapped densities than mucilage, while mucilage had a higher swelling power and a better flow than pectin. Talinum triangulare pectin is a low-methoxyl pectin with a DE of 7.14%. The FTIR spectra showed no interaction between the polymers and ibuprofen. The surface morphology of the microspheres without ibuprofen was smooth, while those with ibuprofen revealed a spongy-like mesh. The swelling power of the microspheres was higher in phosphate buffer with a pH of 7.2 than in distilled water. The entrapment efficiency ranged within 39.57-60.43% w/w, with microspheres containing alginate:mucilage/pectin ratio of 1:1 having higher entrapment efficiency. Microspheres with polymer at a ratio of 1:1 provided a longer release (>2 h), while microspheres with polymer blend of 1:2 provided an immediate release of ibuprofen. CONCLUSIONS: The polymers of T. triangulare could be used as matrices in microsphere formulations.


Assuntos
Ibuprofeno , Pectinas , Pectinas/química , Microesferas , Polímeros/química , Alginatos/química , Tamanho da Partícula , Preparações de Ação Retardada/química
2.
Polim Med ; 52(2): 67-76, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36268745

RESUMO

BACKGROUND: Irvingia gabonensis kernel polymer has gained attention in drug delivery systems because of its compatibility and degradation under natural and physiological conditions. OBJECTIVES: This study aimed to evaluate Irvingia gabonensis polymer as a matrix system for the controlled delivery of ibuprofen in comparison to xanthan gum and hydroxypropylmethylcellulose (HPMC). MATERIAL AND METHODS: Irvingia gabonensis polymer was extracted using established methods and dried using the ovenand freeze-drying methods. Ibuprofen tablets were prepared by direct compression and the effects of polymer concentration (10-50%), excipients (lactose, microcrystalline cellulose and dicalcium phosphate dihydrate) and polymers (xanthan gum and HPMC) on the mechanical and drug release properties of the tablets were evaluated. Density measurements and the Heckel and Kawakita equations were used to determine the compression properties of the tablets. Friability, crushing strength and the crushing strength-friability ratio (CSFR) were used to evaluate the mechanical properties of the tablets, while dissolution times were used to evaluate drug release from the matrices. The drug release mechanisms were determined by fitting the dissolution data into classic kinetic equations. RESULTS: Irvingia gabonensis polymer deformed plastically with a fast onset and a high amount of plastic deformation compared with xanthan gum and HPMC. This polymer was directly compressible and formed intact non-disintegrating tablets; the mechanical and dissolution properties of Irvingia gabonensis polymer tablets generally decreased with increasing concentration of ibuprofen. The ranking of dissolution times was xanthan gum > freeze-dried Irvingia gabonensis > HPMC > oven-dried Irvingia gabonensis. The addition of the excipients improved the mechanical properties of the tablets, aided ibuprofen release, and altered the release kinetics, which was largely defined by the Korsmeyer-Peppas model. Increasing the proportion of xanthan gum and HPMC in the matrices resulted in a decreased amount of ibuprofen released after 9 h, with xanthan gum having a greater effect. CONCLUSIONS: Irvingia gabonensis polymer matrices may be effective in the preparation of controlled release tablets, and their right combination with xanthan gum or HPMC could provide a time-independent release for longer durations.


Assuntos
Ibuprofeno , Polímeros , Excipientes/química , Sistemas de Liberação de Medicamentos , Derivados da Hipromelose , Comprimidos , Preparações de Ação Retardada , Solubilidade
3.
Braz. J. Pharm. Sci. (Online) ; 58: e20263, 2022. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1403679

RESUMO

Abstract The objective of the study was to evaluate the gelling properties of Dillenia indica mucilage in benzyl benzoate emulgel formulation. Mucilage was extracted from the fruits of Dillenia indica using established methods and characterized by rheology and swelling. Emulsion (F1) was prepared using the continental emulsification method. Gelling agents (2 %w /v) were prepared by dispersing in distilled water with constant stirring at a moderate speed using a magnetic stirrer. F1 was added to the gel (0-75 %w /w) to obtain emulgel formulations and evaluated using viscosity, globule size, pH, release profiles and kinetic modeling. Data were expressed as mean ± SD, and similarity factor (f2) was used to compare all formulations. Formulation viscosity was significantly higher with carbopol than with Dillenia; globule sizes increased with concentration of gelling agents, and pH reduced as the concentration of Dillenia increased. All formulations showed controlled release properties with t80 ranging between 114 and 660 min. The release was governed by Korsmeyer-Peppas model. Formulation F5 prepared with 50 % Dillenia showed highest similarity to F4 prepared with 75 %w /w carbopol. Dillenia indica demonstrated acceptable gelling properties comparable with that of carbopol and could be improved for use in emulgel formulations.


Assuntos
Benzoatos/administração & dosagem , Dilleniaceae/anatomia & histologia , Geleificantes , Mucilagem Vegetal/agonistas , Emulsões/análise , Métodos
4.
Braz. J. Pharm. Sci. (Online) ; 58: e19967, 2022. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1384000

RESUMO

Abstract Red lima bean (Phaseolus lunatus Linn) Family Fabaceae, has been modified by succinylation and annealing, and used as intra- and extra-granular disintegrants at concentrations of 5 and 10 %w/w in paracetamol tablet formulation in comparison with corn starch BP. The starches were characterised using FT-IR spectroscopy, SEM, proximate analysis, physicochemical and functional properties. FT-IR spectrometry revealed characteristic peaks at 1575.53 and 1713.99 cm-1 for the succinylated starch while the annealed showed no significant difference from the native starch. Modifications did not alter the ovoid shape of the native starch but reduced the particle size. Succinylation improved water absorption capacity, solubility and swelling of lima bean starch but annealing reduced the parameters. Tablets with disintegrants of lima bean starches generally had higher crushing strengths and lower friability than tablets with corn starch. Modifications reduced the disintegration time of the tablets when the starches were incorporated intra-granularly, which suggested particle-particle bond interruption and destruction of hydrogen bonds as mechanism of disintegration. Tablets containing 10 %w/w succinylated red lima bean starch incorporated intra-granularly had the highest disintegration efficiency ratio, DER, indicating a great balance between mechanical and disintegration properties. Modified red lima bean starches incorporated intra-granularly into paracetamol tablets led to faster disintegration and could efficiently substitute corn starch as disintegrant.


Assuntos
Comprimidos/farmacologia , Abrus/classificação , Amidos e Féculas , Acetaminofen/classificação , Análise Espectral/instrumentação , Espectroscopia de Infravermelho com Transformada de Fourier/métodos
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