Solid Dispersions of Gefitinib Prepared by Spray Drying with Improved Mucoadhesive and Drug Dissolution Properties

Mustafa, Wesam W.; Fletcher, John G.; Khoder, Mouhamad; Alany, Raid G.

doi:10.1208/s12249-021-02187-4

Cited by 24 publications

(18 citation statements)

References 34 publications

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“…However, after being in an alkaline medium (pH 6.8), the three multiparticulate systems showed a more porous structure. Similar studies were carried out by several authors [ 53 , 56 , 61 ]. Therefore, SEM images (pH 6.8) let us assume that the dissolution happens through pores that are generated by a combination of drug diffusion [ 56 ] and polymer swelling/eroding processes [ 53 ].…”

Section: Resultssupporting

confidence: 80%

Multiparticulate Systems of Meloxicam for Colonic Administration in Cancer or Autoimmune Diseases

et al. 2022

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The aim of this research is the development of new colonic release systems of meloxicam (MLX) a non-steroidal anti-inflammatory drug (NSAIDs) with pH and time-dependent vehicles for cancer or autoimmune diseases. The colon has a higher pH than the rest of the gastrointestinal tract (GIT) and this can be used as a modified release strategy. Eudragit® polymers are the most widely used synthetic products in the design of colonic release formulations because they might offer mucoadhesiveness and pH-dependent release. Colonic delivery systems produced with pH-dependent and permeable polymers (FS-30D) or with pH-independent and low permeability polymers (NM-30D), must dissolve at a pH range of 6.0–7.0 to delay the release of the drug and prevent degradation in the GIT, before reaching the colon. The conditions prepared to simulate a gastrointestinal transit showed the CNM multiparticulate system, composed of Eudragit® NM and cellulose, as the best release option for MLX with a more sustained release with respect to the other formulations. CNM formulation followed Higuchi and First-order release kinetics, thus MLX release was controlled by a combination of diffusion and polymers swelling/eroding processes.

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Section: Resultssupporting

confidence: 80%

Multiparticulate Systems of Meloxicam for Colonic Administration in Cancer or Autoimmune Diseases

et al. 2022

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“…The results of FTIR analysis showed that in the spectra of the produced microspheres, the secondary amine sharp peak present in the pure carvedilol disappeared and a broad peak at the same wavenumber range (around 3366.21 cm−1) was observed, which is indicative of formation of hydrogen bond (which is a physical bond) between the O-and NH groups of the drug and polymers 36 . This might be evidence indicating a breakdown in the crystalline structure of carvedilol, leading to the formation of the amorphous state within the microspheres.…”

Section: Discussionmentioning

confidence: 98%

Formulation and Evaluation of Colon Targeted Pulsincap Delivery of Carvedilol for Treatment of Hypertension

Elghamry¹,

Zalat

El-Enin

et al. 2023

Azhar International Journal of Pharmaceutical and Medical Scien

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The objective of this work is to ensure the controlled release of carvedilol at a given time and location for treating hypertension as a pulsincap delivery system. The capsule body was made of insoluble hard gelatin and filled with carvedilol microspheres, then a hydrogel plug was used to close it. The microspheres were made by oil/water emulsification followed by a solvent evaporation method in different drug: polymer ratios using Eudragit L100 and S100 as polymers. Direct compression was used to make the hydrogel plugs. Various assessment parameters, FTIR analysis, and in-vitro release experiments were performed on the produced microspheres. The results showed that formulated microspheres had satisfactory results for various micrometric properties. The microsphere formulations showed the highest entrapment efficiency were F9, F14 and F15 (89.18±2.25, 83.91±2.13 and 92.2±2.28% respectively). FTIR results revealed that carvedilol was molecularly dispersed into the polymeric matrix. In-vitro release studies of carvedilol microspheres showed sustained action over 8 hours. The pulsincap system was evaluated for the in-vitro release studies. PF9 had the highest cumulative release after 12 hours (94.161±0.83 %) and reduced drug release during lag time so, PF9 was chosen for the in-vivo study. The in-vivo study was carried out on 16 hypertensive patients using HPLC method to measure carvedilol conc. in the blood and compare PF9 with commercially available tablets of the same strength. The in-vivo study revealed that the prepared pulsincap has shown better pharmacokinetics parameters compared with the marketed formulation with a delayed release pattern for the effective treatment of hypertension.

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“…36,37 We have investigated the effect of formulation on viability of Caco-2 cells and the results showed that the surfactant used in the solid dispersion formulation is devoid of any cytotoxic effect on Caco-2 cells which is in accordance to a previous report. 29 The improvement in the dissolution profile of cholecalciferol from DRHCap-SD can be attributed to the protection of the cholecalciferol in acidic SGF condition and this can also be associated with the reduction in particle size of the cholecalciferol and its possible amorphization of solid dispersion, enhanced wetting of the drug and the possible solubilization effect of the polymer or surfactant. The bulk properties of the developed solid dispersion and their physical mixture were evaluated and the results demonstrated that the flow properties were improved by formulation of solid dispersion.…”

Section: Discussionmentioning

confidence: 99%

“…It has been demonstrated in the study that the surfactant used in the solid dispersion formulation is devoid of any cytotoxic effect on Caco-2 cells and the observations are in accordance to a previous study. 29…”

Section: Effect Of Formulation On Viability Of Caco-2 Cellsmentioning

confidence: 99%

Delayed Release HPMC Capsules for Efficient Delivery of Cholecalciferol Solid Dispersion

Rawat¹,

Khan²,

Singh³

et al. 2023

Ind. J. Pharm. Edu. Res.

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Introduction:The deficiency of Vitamin D is associated with an increased risk of various diseases and deficiency of this Vitamin is recognized in individuals all over the world. Therefore, the intake of Vitamin D has become essential. Objectives: Cholecalciferol (Vitamin D 3 ) is a poorly soluble molecule and it is very sensitive to degradation under environmental factors such as light, temperature, and oxygen. Its stability is also affected adversely under acidic conditions. Therefore, solid dispersion-based formulation for cholecalciferol was developed and encapsulated in delayed release hydroxypropylmethyl cellulose (HPMC) capsules. Materials and Methods: Cholecalciferol solid dispersion was developed and characterized by Fourier transform-infra red spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and X-ray diffraction analysis. The effect of various concentrations of cholecalciferol formulations on the viability of Caco-2 cells was determined by using MTT assay. Dissolution profile and stability study of the developed product was also evaluated. Results: The results demonstrated improved solubility of cholecalciferol in solid dispersion-based formulation. The drug content of solid dispersions was in the order of 91±2.3% and various studies showed the amorphous form of cholecalciferol in the solid dispersion. The cell viability assay in Caco-2 cells demonstrated that the surfactant used in the solid dispersion formulation of cholecalciferol had no adverse effect on intestinal cells. Further, dissolution profile of HPMC capsule encapsulated solid dispersion showed improved dissolution of cholecalciferol. Moreover, the stability study indicated no significant changes in the cholecalciferol content in the developed formulation under storage at experimental conditions. Conclusion: The solid dispersion-based formulation of cholecalciferol exhibited improved solubility and found to be compatible with Caco-2 cells. The delayed release HPMC capsule encapsulated solid dispersion of cholecalciferol (DRHCap-SD) showed improved dissolution and acceptable stability profile and this represent a potential delivery system for oral administration of cholecalciferol.

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Solid Dispersions of Gefitinib Prepared by Spray Drying with Improved Mucoadhesive and Drug Dissolution Properties

Cited by 24 publications

References 34 publications

Multiparticulate Systems of Meloxicam for Colonic Administration in Cancer or Autoimmune Diseases

Multiparticulate Systems of Meloxicam for Colonic Administration in Cancer or Autoimmune Diseases

Formulation and Evaluation of Colon Targeted Pulsincap Delivery of Carvedilol for Treatment of Hypertension

Delayed Release HPMC Capsules for Efficient Delivery of Cholecalciferol Solid Dispersion

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