Preparation and In Vitro/Vivo Evaluation of New Celecoxib Solid Dispersions with Co-Carrier Containing Aerosil and Poloxamer 188

Shi, Xiangjun; Ding, Zejie; Bao, Jiayin; Wang, Chao

doi:10.1007/s11094-021-02316-0

Cited by 3 publications

(1 citation statement)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Furthermore, the presence or coating of poloxamer ® 188 also provides a gastroprotective effect [ 18 ] and significantly improves the intestinal absorption of the drug [ 19 ]. As per the literature, poloxamer ® 188 is frequently used as a hydrophilic carrier along other carriers for the development of TSD [ 20 , 21 , 22 , 23 , 24 ].…”

Section: Introductionmentioning

confidence: 99%

In Vitro and Biological Evaluation of Oral Fast-Disintegrating Films Containing Ranitidine HCl and Syloid® 244FP-Based Ternary Solid Dispersion of Flurbiprofen

Rashid,

Irfan,

Kamal

et al. 2024

Pharmaceutics

View full text Add to dashboard Cite

Flurbiprofen (FBP), a nonsteroidal anti-inflammatory drug (NSAID), is commonly used to treat the pain of rheumatoid arthritis, but in prolonged use it causes gastric irritation and ulcer. To avoid these adverse events of NSAIDs, the simultaneous administration of H2 receptor antagonists such as ranitidine hydrochloride (RHCl) is obligatory. Here, we developed composite oral fast-disintegrating films (ODFs) containing FBP along with RHCl to provide a gastroprotective effect as well as to enhance the solubility and bioavailability of FBP. The ternary solid dispersion (TSD) of FBP was fabricated with Syloid® 244FP and poloxamer® 188 using the solvent evaporation technique. The synthesized FBP-TSD (coded as TSD) was loaded alone (S1) and in combination with plain RHCl (S2) in the composite ODFs based on hydroxypropyl methyl cellulose E5 (HPMC E5). The synthesized composite ODFs were evaluated by in vitro (thickness, folding endurance, tensile strength, disintegration, SEM, FTIR, XRD and release study) and in vivo (analgesic, anti-inflammatory activity, pro-inflammatory cytokines and gastroprotective assay) studies. The in vitro characterization revealed that TSD preserved its integrity and was effectively loaded in S1 and S2 with optimal compatibility. The films were durable and flexible with a disintegration time ≈15 s. The release profile at pH 6.8 showed that the solid dispersion of FBP improved the drug solubility and release when compared with pure FBP. After in vitro studies, it was observed that the analgesic and anti-inflammatory activity of S2 was higher than that of pure FBP and other synthesized formulations (TSD and S1). Similarly, the level of cytokines (TNF-α and IL-6) was also markedly reduced by S2. Furthermore, a gastroprotective assay confirmed that S2 has a higher safety profile in comparison to pure FBP and other synthesized formulations (TSD and S1). Thus, composite ODF (S2) can effectively enhance the FBP solubility and its therapeutic efficacy, along with its gastroprotective effect.

show abstract

Section: Introductionmentioning

confidence: 99%

In Vitro and Biological Evaluation of Oral Fast-Disintegrating Films Containing Ranitidine HCl and Syloid® 244FP-Based Ternary Solid Dispersion of Flurbiprofen

Rashid,

Irfan,

Kamal

et al. 2024

Pharmaceutics

View full text Add to dashboard Cite

show abstract

Co-carrier-based solid dispersion of celecoxib improves dissolution rate and oral bioavailability in rats

Tran

Nguyen

Park

2023

Journal of Drug Delivery Science and Technology

View full text Add to dashboard Cite

Dexamethasone Acetate Nanocrystals, Characterization and Dissolution Studies in Presence of Polymorphic Phases

Bastos

Barbosa

Silva

et al. 2023

PNT

View full text Add to dashboard Cite

Background: A drug with poor water-solubility, like Dexamethasone acetate, can present lower bioavailability conventional for pharmaceutical formulations, and the presence of polymorphs in the raw material can lead to drug quality problems. background: Nanocrystals of dexamethasone acetate were synthesized by high pressure homogenizer (HPH) method in surfactant poloxamer 188 (P188) solid dispersion Objective: In this study, nanocrystals of dexamethasone acetate were synthesized by high pressure homogenizer (HPH) method in surfactant poloxamer 188 (P188) solid dispersion and the bioavailable in raw material with polymorphism presence was evaluated. objective: The main purposes of this study were (a) to obtain nanocrystals of dexamethasone acetate by HPH process in polymer P188 solid dispersion, (b) to correlate physicochemical properties with particle size and of physical mixture of polymorphs in raw material, and (c) to evaluate the influence of these formulation in dissolution rate of this drug. Methods: The powder pre-suspension was prepared by the HPH process, and the nanoparticles formed were incorporated in P188 solutions. The nanocrystals formed were characterized by techniques of XRD, SEM, FTIR, thermal analysis by differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA), dynamic light scattering (DLS) to analyze the particle size and zeta potential, and in vitro evaluation by dissolution studies. method: The powder pre-suspension was prepared by the HPH process and the nanoparticles formed were incorporated in P188 solutions. The nanocrystals formed were characterized by techniques of XRD, SEM, FTIR, thermal analysis by differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA), dynamic light scattering (DLS) to analyze the particle size and zeta potential, and in vitro evaluation by dissolution studies. Results: The characterization techniques were adequate to show the presence of raw material with physical moisture between two dexamethasone acetate polymorphs. The nanocrystals formed in the presence of the P188 in the formulation showed a considerable increase in the rate of dissolution of the drug in the medium and in the size of the stable nanocrystals, even in the presence of dexamethasone acetate polymorphs. Conclusion: The results showed that it was possible to produce dexamethasone nanocrystals by HPH process with regular size by the presence of the small amount of P188 surfactant. This article presents a novelty in the development of dexamethasone nanoparticles that have different polymorphic forms in their physical composition.

show abstract

Preparation and In Vitro/Vivo Evaluation of New Celecoxib Solid Dispersions with Co-Carrier Containing Aerosil and Poloxamer 188

Cited by 3 publications

References 27 publications

In Vitro and Biological Evaluation of Oral Fast-Disintegrating Films Containing Ranitidine HCl and Syloid® 244FP-Based Ternary Solid Dispersion of Flurbiprofen

In Vitro and Biological Evaluation of Oral Fast-Disintegrating Films Containing Ranitidine HCl and Syloid® 244FP-Based Ternary Solid Dispersion of Flurbiprofen

Co-carrier-based solid dispersion of celecoxib improves dissolution rate and oral bioavailability in rats

Dexamethasone Acetate Nanocrystals, Characterization and Dissolution Studies in Presence of Polymorphic Phases

Contact Info

Product

Resources

About