Development and optimisation of simulated salivary fluid for biorelevant oral cavity dissolution

Ali, Joseph; Lee, Jong Bong; Gittings, Sally; Iachelini, Alessandro; Bennett, Joanne; Cram, Anne; Garnett, Martin C.; Roberts, Clive J.; Gershkovich, Pavel

doi:10.1016/j.ejpb.2021.01.017

Cited by 21 publications

(10 citation statements)

References 84 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…An in vitro study was conducted to test unidirectional and bidirectional tablets’ swelling index (SI). Simulated salivary fluid (SSF), composed of mineral salts, Tween ® 20 and xanthan gum [ 32 ], was used for the assay. Each tablet was weighed and put into a beaker containing 5 mL of SSF.…”

Section: Methodsmentioning

confidence: 99%

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

et al. 2022

View full text Add to dashboard Cite

A pharmaceutical vehicle based on lyophilized liposomes is proposed for the buccal administration of drugs aimed at systemic delivery through the sublingual mucosa. Liposomes made of egg phosphatidylcholine and cholesterol (7/3 molar ratio) were prepared and lyophilized in the presence of different additive mixtures with mucoadhesive and taste-masking properties. Palatability was assayed on healthy volunteers. The lyophilization cycle was optimized, and the lyophilized product was compressed to obtain round and capsule-shaped tables that were evaluated in healthy volunteers. Tablets were also assayed regarding weight and thickness uniformities, swelling index and liposome release. The results proved that lyophilized liposomes in unidirectional round tablets have palatability, small size, comfortability and buccal retention adequate for sublingual administration. In contact with water fluids, the tablets swelled, and rehydrated liposomes were released at a slower rate than permeation efficiency determined using a biomimetic membrane. Permeability efficiency values of 0.72 ± 0.34 µg/cm2/min and 4.18 ± 0.95 µg/cm2/min were obtained for the liposomes with and without additives, respectively. Altogether, the results point to the vehicle proposed as a liposomal formulation suitable for systemic drug delivery through the sublingual mucosa.

show abstract

Section: Methodsmentioning

confidence: 99%

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

et al. 2022

View full text Add to dashboard Cite

show abstract

“…SM FMTs dissolution was proceeded via the USP dissolution system, Distek (Model 2500i Type II, TCS-0500 Scheduler, New Jersey, USA) at 37 ± 0.5oC and at 50 rpm using 900 mL of SSF as the dissolution medium (Moqbel et al., 2016 ; Shohin et al., 2016 ; Fouad et al., 2020 ; AlAli et al., 2021 ; Ali et al., 2021 . Samples were taken at (2, 4, 6, 8, 10, 20 and 30 min), 5 mL aliquots samples were withdrawn and instantaneously replaced with 5 mL SSF kept at the same temperature (Cirri et al., 2005 ; Sheta & Boshra, 2021 ).…”

Section: Methodsmentioning

confidence: 99%

Design and optimization of silymarin loaded in lyophilized fast melt tablets to attenuate lung toxicity induced via HgCl₂ in rats

et al. 2022

View full text Add to dashboard Cite

The present study aimed to develop fast melting tablets (FMTs) using silymarin (SM) owing to FMTs rapid disintegration and dissolution. FMTs represent a pathway to help patients to increase their compliance level of treatment via facile administration without water or chewing beside reduction cost. One of the methods for FMTs formulation is lyophilization. Optimization of SM-FMTs was developed via a 3 2 factorial design. All prepared SM-FMTs were evaluated for weight variation, thickness, breaking force, friability, content uniformity, disintegration time (DT), and % SM released. The optimized FMT formula was selected based on the criteria of scoring the fastest DT and highest % SM released after 10 min (Q 10 ). Optimized FMT was subjected to Fourier transform infrared spectroscopy (FT-IR), X-ray powder diffraction (XRD), and scanning electron microscopy (SEM) besides investigating its lung-protective efficacy. All SM-FMT tablets showed acceptable properties within the pharmacopeial standards. Optimized FMT (F7) scored a DT of 12.5 ± 0.64 Sec and % SM released at Q 10 of 82.69 ± 2.88%. No incompatibilities were found between SM and excipients, it showed a porous structure under SEM. The optimized formula decreased cytokines, up-regulated miRNA133a, and down-regulated miRNA-155 and COX-2 involved in the protection against lung toxicity prompted by HgCl 2 in a manner comparable to free SM at the same dosage.

show abstract

“…In vitro drug release studies were conducted in simulated saliva, based on a previously published method [ 61 ]. Briefly, supersaturation studies were performed in small-scale glass vials (1.5 mL maximum volume) under stirring.…”

Section: Methodsmentioning

confidence: 99%

Preparation and Evaluation of Amorphous Solid Dispersions for Enhancing Luteolin’s Solubility in Simulated Saliva

2022

View full text Add to dashboard Cite

Luteolin (LUT), a bioactive flavonoid, possesses various pharmacological properties, including antioxidant, antimicrobial, anti-allergic, cardio-protective, and anti-cancer activity. Among them, LUT’s administration for the treatment of periodontal disease is very promising. However, its low water solubility magnifies the challenge of formulating LUT into an effective dosage form. In this vein, the aim of the present study examines the preparation of amorphous solid dispersions (ASD) for the solubility improvement of LUT in saliva. At first, the physicochemical properties of the active pharmaceutical ingredient (API) were studied before the selection of the most suitable ASD matrix/carrier. For this reason, six commonly used polymeric ASD matrix/carriers (namely, povidone, PVP; copovidone, coPVP; hydroxypropyl cellulose, HPC-SL; hydroxypropyl methyl cellulose acetate succinate, HPMC-AS; Eudragit® RS, Eud-RS; and Soluplus®, SOL) were screened via the film casting method, as to whether they could suspend the drug’s recrystallization. The most promising matrix/carriers were then evaluated, based on their ability to inhibit LUT’s precipitation after its solubilization, via the solvent shift method. Based on both screening methods, it was determined that PVP was the most promising matrix/carrier for the preparation of LUT’s ASDs. Hence, in a further step, after the successful testing of components’ miscibility, LUT–PVP ASDs were prepared via the solvent evaporation method. These systems (examined via powder X-ray diffractometry, pXRD) showed full API amorphization immediately after preparation and excellent physical stability (since they were stable after 3 months of storage). The study of LUT–PVP ASD’s ATR-FTIR (Attenuated Total Reflectance-Fourier Transform Infrared) spectra demonstrated strong H-bonds between the molecules of the drug and the matrix/carrier, while molecular dynamics (MD) simulations were able to shed light on these drug–matrix/carrier interactions, at a molecular level. Finally, in vitro dissolution studies in simulated saliva proved that the prepared ASDs were able to significantly enhance LUT’s dissolution profile. Hence, according to findings of the present work, the preparation of LUT-ASDs utilizing PVP as the polymeric matrix/carrier is regarded as a highly promising technique for the improvement of API’s solubility in the oral cavity.

show abstract

Development and optimisation of simulated salivary fluid for biorelevant oral cavity dissolution

Cited by 21 publications

References 84 publications

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

Design and optimization of silymarin loaded in lyophilized fast melt tablets to attenuate lung toxicity induced via HgCl₂ in rats

Preparation and Evaluation of Amorphous Solid Dispersions for Enhancing Luteolin’s Solubility in Simulated Saliva

Contact Info

Product

Resources

About

Development and optimisation of simulated salivary fluid for biorelevant oral cavity dissolution

Cited by 21 publications

References 84 publications

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

Development of a Mucoadhesive Vehicle Based on Lyophilized Liposomes for Drug Delivery through the Sublingual Mucosa

Design and optimization of silymarin loaded in lyophilized fast melt tablets to attenuate lung toxicity induced via HgCl2 in rats

Preparation and Evaluation of Amorphous Solid Dispersions for Enhancing Luteolin’s Solubility in Simulated Saliva

Contact Info

Product

Resources

About

Design and optimization of silymarin loaded in lyophilized fast melt tablets to attenuate lung toxicity induced via HgCl₂ in rats