Ferulic acid's therapeutic odyssey: nano formulations, pre-clinical investigations, and patent perspective.

INTRODUCTION: Ferulic acid (FA) is a phenolic phytochemical that has garnered the attention of the research community due to its abundant availability in nature. It is a compound that has been explored for its multifaceted therapeutic potential and benefits in modern and contemporary healthcare. AREAS COVERED: This review furnishes a compilation of the molecular mechanisms underlying the anti-diabetic, anticancer, antioxidant, and anti-inflammatory effects of FA. We also aim to excavate an in-depth analysis of the role of nanoformulations to achieve release control, reduce toxicity, and deliver FA at specified target sites. To corroborate the safety and efficacy of FA, a multitude of pre-clinical studies have also been conducted by researchers and have been discussed comprehensively in this review. The various patented innovations and newer paradigms pertaining to FA have also been presented. EXPERT OPINION: Enormous research has been conducted and should still be continued to find the best possible novel drug delivery system for FA delivery. The utilization of nanocarriers and nanoformulations has intrigued the scientists for delivery of FA, but before that, it is necessary to shed light upon toxicity, safety, and regulatory concerns of FA.

Talinum triangulare (Jacq.) Willd. mucilage and pectin in the formulation of ibuprofen microspheres.

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.

Irvingia gabonensis (O'Rorke) Bail polymer matrix system for controlled drug delivery.

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.

Intra and Extra-granular Disintegrant Properties of Modified Underutilised Red Lima Bean Starch in Paracetamol Tablet Formulation

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.

Evaluation of starch-clay composites as a pharmaceutical excipient in tramadol tablet formulations.

BACKGROUND: Co-processing starch with clay nanocomposite has been shown to yield a new class of materials, potentially with better properties than pristine starch, that could be used as directly compressible excipients in tablet formulations. OBJECTIVES: In this study, starches from 3 botanical sources, i.e., millet starch from Pennistum glaucum (L) RBr grains, sorghum starch from Sorghum bicolor L. Moench grains and cocoyam starch from Colocasia esculenta L. Schott tubers, were co-processed with montmorillonite clay (MMT) and evaluated as a directly compressible excipient in tramadol tablet formulations. The effects of different starch-to-clay ratios on the material and drug release properties of the resulting tablets were evaluated. MATERIAL AND METHODS: The starch-clay composites were prepared by heating a dispersion of the starch in distilled water, then precipitating the dispersion with an equal volume of 95% ethanol. The starch-clay composites were characterized and used as direct compression excipients for the preparation of tramadol tablets. The mechanical and drug release properties of the tablets were evaluated. RESULTS: Co-processing MMT with the starches yielded starch-clay composites with different material and tablet properties than the pristine starches. The co-processed starch-MMT biocomposites exhibited improved flowability and compressibility over the pristine starches. The mechanical and drug release properties of tramadol tablets containing starch-clay composites were significantly better than those containing only pristine starches. The properties of the starch-clay composites were not related to the botanical source of the starches. CONCLUSIONS: The study showed that starch-clay biocomposites could be used in the controlled release of tramadol.

Film forming properties of Cissus pulpunea (Guill and Perr) and Irvingia gabonensis (O'Rorke) gums.

BACKGROUND: Natural polymers such as gums have gained attention in drug delivery systems due to their availability, compatibility and degradation under natural and physiological conditions. OBJECTIVES: The aim of the present study was to investigate the film forming properties of gums obtained from the stem of Cissus polpunea (Guill and Perr) and the seed of Irvingia gabonensis (O'Rorke). MATERIAL AND METHODS: Gums were extracted from the relevant plant parts and characterized using functional, proximate and elemental properties. Films were prepared by the casting method using gum concentrations of 1-4% w/v and varied with propylene glycol (PG). The films were assessed through physical observation, thickness, swelling power and moisture sorption effects using the relative humidity of 0, 27, 43, 57, 75 and 90%. The gum yielding optimal film properties was used as coating material in ibuprofen tablet formulations. The mechanical and release properties of the tablets were determined. RESULTS: The functional and proximate properties of gums showed a similarity in the majority of the parameters, but significant (p < 0.05) variation existed in their solubility, while elemental assessment revealed the absence of toxic metals. Generally, the films were homogenous, opaque and demonstrated high swelling power in phosphate buffer, which was pH-dependent. Moisture sorption properties of the gums increased with the increase in relative humidity in the order HPMC < Cissus < Irvingia. Film-coated ibuprofen tablets showed higher mechanical properties and disintegration and dissolution times compared with uncoated tablets. CONCLUSIONS: Cissus and irvingia gums have demonstrated acceptable functional, proximate and elemental properties. Film-coated ibuprofen tablets showed higher mechanical and release properties than was the case in uncoated tablets.

Influence of binder type and process parameters on the compression properties and microbial survival in diclofenac tablet formulations

The influence of binder type and process parameters on the compression properties and microbial survival in diclofenac tablet formulations were studied using a novel gum from Albizia zygia. Tablets were produced from diclofenac formulations containing corn starch, lactose and dicalcium phosphate. Formulations were analyzed using the Heckel and Kawakita plots. Determination of microbial viability in the formulations was done on the compressed tablets of both contaminated and uncontaminated tablets prepared from formulations. Direct compression imparted a higher plasticity on the materials than the wet granulation method. Tablets produced by wet granulation presented with a higher crushing strength than those produced by the direct compression method. Significantly higher microbial survival (p< 0.05) was obtained in formulations prepared by direct compression. The percent survival of Bacillus subtilis spores decreased with increase in binder concentration. The study showed that Albizia gum is capable of imparting higher plasticity on materials and exhibited a higher reduction of microbial contaminant in the formulations. The direct compression method produced tablets of reduced viability of microbial contaminant.

A influência do tipo de ligante e os parâmetros do processo de propriedades de compressão e sobrevivência microbiana em comprimidos de diclofenaco foram estudados utilizando uma nova goma de Albizia zygia. Os comprimidos foram produzidos a partir de formulações de diclofenaco contendo amido de milho, lactose e fosfato bicálcico. As formulações foram analisadas usando os gráficos de Heckel e Kawakita. A determinação da viabilidade microbiana nas formulações foi feita nos comprimidos contaminados e não contaminados preparados a partir de formulações. A compressão direta confere maior plasticidade dos materiais do que o método de granulação úmida. Comprimidos produzidos por granulação úmida apresentaram maior força de esmagamento do que aqueles produzidos pelo método de compressão direta. Observou-se sobrevivência significativamente maior (p<0,05) em formulações preparadas por compressão direta. A sobrevivência percentual dos esporos de Bacillus subtilis diminuiu com o aumento da concentração do agregante. O estudo mostrou que a goma de Albizia é capaz de conferir maior plasticidade aos materiais e apresentou maior redução da contaminação microbiana nas formulações. O método de compressão direta produziu comprimidos com viabilidade reduzida de contaminantes microbianos.