An Overview of Pharmaceutical Excipients: Safe or Not Safe?

Abrantes, Cátia G.; Duarte, Dinah; Reis, Catarina Pinto

doi:10.1016/j.xphs.2016.03.019

Cited by 96 publications

(53 citation statements)

References 51 publications

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“…As most of these approaches led to low-to-moderate success (Hatanaka, Kimura, Lai-Fu, Onoue, & Yamada, 2008;Piao et al, 2011;Zhou et al, 2013), new strategies, especially green ones (Chemat et al, 2017), are in great demand, aiming not only to increase the solubility of CoQ10, but also to eliminate the use of any surfactant or organic solvent. These chemical additives are frequently employed to deal with hydrophobic compounds; however, most of which are not inert from the perspective of pharmaceutical product quality and lead to a variety of vehiclerelated side effects (Abrantes, Duarte, & Reis, 2016). Hence, green approaches are of undeniable value, especially when it comes to supplements that are generally recommended for daily use.…”

Section: Introductionmentioning

confidence: 99%

Green Formulation of Triglyceride/Phospholipid‐Based Nanocarriers as a Novel Vehicle for Oral Coenzyme Q10 Delivery

Alavi

Akhlaghi

Dadashzadeh

et al. 2019

Journal of Food Science

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This study was aimed to develop a novel nanocarrier for coenzyme Q10 (CoQ10) by a green process that prevented the use of surfactants and organic solvents. Triglyceride/phospholipid‐based nanocarriers were developed through high‐pressure homogenization (an industrial feasible process), and a 25‐1 fractional factorial design was adopted to assess the influences of formulation variables on the considered responses, including vesicle size, entrapment efficiency, loading capacity, and solubility of the vehicles in simulated gastrointestinal fluids. The optimized formulation was further in‐depth characterized in terms of morphology, release behavior, biocompatibility (Caco‐2 cell cytotoxicity and histological examination), thermal behavior, and Fourier transform infrared analysis. Optimal nanocarriers were found to have mean particle size of 75 nm, narrow particle distribution, and CoQ10 entrapment of 95%. The optimized formulation was stable upon incubation in simulated gastrointestinal fluids without considerable leakage of cargo, which was in agreement with their sustained release behavior. Microscopic observations also confirmed nanosized nature of the vesicles and revealed their spherical shape. Moreover, toxicity evaluations at the cellular and tissue levels revealed their nontoxic nature. In conclusion, triglyceride/phospholipid‐based nanocarriers proved to be a green safe vehicle for delivery of CoQ10 with industrial‐scale production capability and could provide a new horizon for delivery of hydrophobic nutraceuticals. Practical application Green nanostructure formulation approaches have recently gained tremendous attraction for their safe profile especially when it comes to supplements, which are generally recommended for daily use. However, their sufficient association with cargoes and industrial‐scale production have remained considerable challenges. This study focuses on the development of lipid‐based nanocarriers for CoQ10 by an industrial feasible process that prevents the use of any surfactants or organic solvents.

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Section: Introductionmentioning

confidence: 99%

Green Formulation of Triglyceride/Phospholipid‐Based Nanocarriers as a Novel Vehicle for Oral Coenzyme Q10 Delivery

Alavi

Akhlaghi

Dadashzadeh

et al. 2019

Journal of Food Science

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“…[27][28][29][30] These interactions may lead to altered absorption, distribution, metabolism and elimination of an API, ultimately affecting its bioavailability. [31,32] Not only is it possible to establish pharmacokinetic effects of extract/excipient combinations, one could furthermore determine whether the excipients altered effects induced by the respective extracts, indicating possible physicochemical interactions and aid in safe future oral pharmaceutical formulation of said extracts. For this purpose, standard cell viability assays (MTT; LDH) and flow cytometric analysis for the determination of apoptosis by means of annexin V/PI staining were performed.…”

Section: Introductionmentioning

confidence: 99%

In -vitro cytotoxicity of various Siphonochilus aethiopicus (Schweinf.) B.L. Burtt extracts in combination with selected tableting excipients

Erasmus

Plessis

Viljoen

2019

Journal of Pharmacy and Pharmacology

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Objectives To investigate the cytotoxic potential of S. aethiopicus extracts in combination with chitosan and Pharmacel®101, on two cell lines. Methods Extracts were chemically characterised utilising UPLC‐Q‐TOF/MS, followed by determination of cell viability and membrane integrity. Key findings Ethanol (EtOH) and diethyl ether (DiEt) extracts contained significant quantities of all chosen biomarker molecules; however, only two were scarcely quantifiable in aqueous extracts. Aqueous extracts did not induce any cytotoxic effects, whereas EtOH and DiEt extracts caused concentration‐dependent decreases in cell viability and membrane integrity loss in both cell lines. Ensuing exposure to EtOH extracts at 50, 100 and 150 μg/ml, HepG2 cells were considered 15.5%, 12.5% and 32.8% apoptotic, whereas DiEt extracts caused 4.5%, 13.5% and 33.9% apoptotic cells. Exposure to EtOH and DiEt extracts at 50 μg/ml ensued in 20.2% and 21.3% apoptosis in Caco‐2 cells; 100 μg/ml induced apoptosis in 19.9% and 10.3% of Caco‐2 cells; whereas exposure to 150 μg/ml EtOH extracts caused 12.6% apoptosis compared to 11.7% induced by the DiEt extract. Conclusions None of the excipients caused any significantly altered cellular effects, indicating little chance for physicochemical interactions. Aqueous extracts did not possess any cytotoxic properties. However, it is clear that organic extracts caused apoptotic and necrotic cell death.

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“…(1)(2) The excipients also influence in a significative fashion the release of the active principle contained in the medicine. (3)(4) During the production process, the intrinsic characteristics of the (solid state) excipients as well as of the active principle are reflected in important parameters of the tablets, such as compressibility, fluidity, ability to form uniform mixtures, lubrication, sedimentation and solubility. (5)(6) More and more, excipients are gaining increasing prominence within pharmaceutical formulations, assuming now multiple functions critical to the effectiveness, safety and stability of the dosage forms.…”

Section: Introductionmentioning

confidence: 99%

Bran of cassava starch flour and bran of cassava flour as potential tablet excipients

et al. 2019

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Objectives:The physicochemical characteristics of bran of cassava starch flour and bran of cassava flour (viz. organoleptic characteristics, pH value, moisture content, total ashes, lipid, protein, starch and fiber contents) and biopharmacotechnical parameters (viz. granulometry, flow capacity, angle at rest, outflow time and apparent density) were evaluated aiming at assessing their potential use as tablet excipients.Methodos: Three tablet formulations of venlafaxine hydrochloride were proposed, having as excipients bran of cassava flour, bran of cassava starch flour and Starch 1500 ® . The tablets were produced using two different pressures (98±5 MPa and 32±6 Mpa) and their mechanical (hardness and friability) and dissolubility characteristics were evaluated. Results and Conclusions:The tablets produced with both cassava flours, using higher pressures, presented similar physicochemical characteristics to those obtained with the excipient Starch1500 ® , thus indicating that cassava flours possess the potential to be used as disintegrating agents in tablets. RESUMENObjetivos: Se evaluaron características físico-químicas del salvado de harina y del salvado de la fécula de mandioca (características organolépticas, pH, humedad, cenizas totales y contenido de lípidos, proteínas, almidones y fibras) y biofarmacotécnicas (granulometría, capacidad de flujo, ángulo en reposo, tiempo de salida y densidad aparente) con el objetivo de evaluar el uso de estos residuos como excipientes para comprimidos.Métodos: Se propusieron tres formulaciones en comprimidos de venlafaxina teniendo como excipientes salvado de harina de mandioca, salvado de fécula de mandioca y Starch 1500 ®. Las pastillas se produjeron utilizando dos presiones diferentes (98 ± 5 MPa y 32 ± 6 Mpa). Las características mecánicas (dureza y friabilidad) y de disolución de los comprimidos se evaluaron. Resultados y Conclusiones:Los comprimidos producidos con ambos salvados de mandioca, utilizando las presiones más elevadas, presentaron características físico-químicas similares a las obtenidas con el excipiente Starch1500®, indicando que las harinas de mandioca poseen potencial para ser utilizadas como agentes desintegrantes en comprimidos.

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An Overview of Pharmaceutical Excipients: Safe or Not Safe?

Cited by 96 publications

References 51 publications

Green Formulation of Triglyceride/Phospholipid‐Based Nanocarriers as a Novel Vehicle for Oral Coenzyme Q10 Delivery

Green Formulation of Triglyceride/Phospholipid‐Based Nanocarriers as a Novel Vehicle for Oral Coenzyme Q10 Delivery

In -vitro cytotoxicity of various Siphonochilus aethiopicus (Schweinf.) B.L. Burtt extracts in combination with selected tableting excipients

Bran of cassava starch flour and bran of cassava flour as potential tablet excipients

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