Formulation and biopharmaceutical evaluation of bitter taste masking microparticles containing azithromycin loaded in dispersible tablets

Tung, Nguyen-Thach; Tran, Cao-Son; Nguyen, Tran-Linh; Hoang, Tung; Trinh, T.S.; Nguyen, Thi-Ngan

doi:10.1016/j.ejpb.2017.03.017

Cited by 24 publications

(11 citation statements)

References 46 publications

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“…The exact reasons for this low oral bioavailability are not specified. However, many reports are suggesting that it might be attributed to different factors such as the low aqueous solubility (AZM is practically insoluble in water) which may lead to erratic dissolution rates [11][12][13][14][15], the drug relatively high molecular weight, the low stability at the acidic gastric pH (AZM have a high potential of decomposition in acidic medium) [16], and the incomplete gastrointestinal tract (GIT) absorption [17]. Pharmacokinetically, most poorly water-soluble drugs have low bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

et al. 2020

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Azithromycin (AZM) is a macrolide antibiotic used for the treatment of various bacterial infections. The drug is known to have low oral bioavailability (37%) which may be attributed to its relatively high molecular weight, low solubility, dissolution rate, and incomplete intestinal absorption. To overcome these drawbacks, liquid (L) and solid (S) self-emulsifying drug delivery systems (SEDDs) of AZM were developed and optimized. Eight different pseudo-ternary diagrams were constructed based on the drug solubility and the emulsification studies in various SEDDs excipients at different surfactant to co-surfactant (Smix) ratios. Droplet size (DS) < 150 nm, dispersity (Đ) ≤ 0.7, and transmittance (T)% > 85 in three diluents of distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF) were considered as the selection criteria. The final formulations of L-SEDDs (L-F1(H)), and S-SEDDs (S-F1(H)) were able to meet the selection requirements. Both formulations were proven to be cytocompatible and able to open up the cellular epithelial tight junctions (TJ). The drug dissolution studies showed that after 5 min > 90% and 52.22% of the AZM was released from liquid and solid SEDDs formulations in DW, respectively, compared to 11.27% of the pure AZM, suggesting the developed SEDDs may enhance the oral delivery of the drug. The formulations were stable at refrigerator storage conditions.

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Section: Introductionmentioning

confidence: 99%

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

et al. 2020

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“…It has been reported by World Health Organization (WHO) that there are approximately 300–500 million people who had suffered from trachoma [1]. Azithromycin (AZI) is a new type of semi-synthetic macrolide antibiotic, which shows antibacterial effects to a variety of common pathogenic bacteria and has been used to treat respiratory infections, skin and soft-tissue infections and genital infections [2]. Previous reports have demonstrated that the oral dosage forms of azithromycin were effective for the treatment of eye infections, such as conjunctivitis and other sensitive pathogens [3,4,5].…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Topically Applied Azithromycin Based on Sodium Hyaluronate in Treatment of Conjunctivitis

Chen

Yin

et al. 2019

Pharmaceutics

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Azithromycin (AZI) eye drops containing sodium hyaluronate (SH) were developed to improve the bioavailability of AZI. Interaction between AZI and SH in the AZI-SH formulation was investigated by differential scanning calorimetry, X-ray diffraction, and 1H-nuclear magnetic resonance spectroscopy analyses. Moreover, advantages of using SH as an excipient were investigated by comparing physiological properties and pharmacokinetic behaviors of SH-containing AZI eye drops with that of hydroxypropyl methylcellulose (HPMC)-containing formulation. In addition, safety of the developed AZI-SH eye drops was evaluated by in vitro 3-(4,5-dimethyl-2-Thiazyl)-2, 5-diphenyl-2H-tetrazolium bromide assay (MTT assay) and neutral red uptake assay as well as in vivo eye irritation test and acute toxicity test. The results indicated that AZI formed a complex with SH under a slightly acidic condition. The area under the curve (AUC) of AZI in SH-containing formulation was 1.58-fold higher (P<0.01) than that in HPMC-containing formulation due to the interaction between the amine group of AZI and the carboxyl group of SH, despite of the higher viscosity of HPMC-containing formulation. Safety evaluation showed that AZI-SH eye drops caused no obvious eye irritation and acute toxicity. In conclusion, the developed SH-containing AZI formulation possessing advantages of longer retention time and higher drug availability was a promising drug formulation for topical ocular therapy.

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“…First, Azithromycin has been known as a weakly basic drug thus having higher solubility in an acidic medium. However, according to our previous study 34 , this drug was found unstable in very low pH medium such as pH 1-3, thus pH between 4 and 5 would be considered. At the same time, Eudragit EPO is completely soluble in an acidic dissolution medium (pH 4.5) and is not soluble at pH over 5-6.…”

Section: Characterization Of Azithromycin Nanoparticlesmentioning

confidence: 99%

Evaluation of formulation variables on azithromycin nanoparticles prepared by emulsification solvent diffusion method using quality by design approach

Tung¹,

Nguyen²,

Nguyen³

2022

Pharm Sci Asia

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The study aims to investigate the effect of formulation variables on the characteristics of azithromycin (AZI) nanoparticles using a quality by design approach. AZI nanoparticles were prepared by the emulsification solvent diffusion method. Two critical factors, the ratio of AZI: Eudragit EPO (X1) and volume of outer aqueous medium (X2), were chosen as independent variables for central composite design. The optimized formulation was further characterized by Fourier transform infrared spectroscopy, X-ray diffractometry, transmission electron microscopy, and dissolution test. The obtained results showed variability of mean particle size, entrapment efficacy, and zeta potential from 200 to 1232 nm, 10.78 to 75.9%, and 31 to 43 mV, respectively. The main coefficients indicated that the ratio of AZI: polymer (X1) possessed a synergistic effect on mean particle size (Y1), and volume of outer aqueous medium (X2) had an antagonistic effect on particle size. The interaction between the ratio of AZI: Eudragit EPO (X1) and volume of outer aqueous medium (X2) exhibited a significant antagonistic effect on entrapment efficacy (Y2) (p<0.05). AZI existed in an amorphous state in nanoparticles that were spherical and homogeneous in shape. The nanoparticles revealed the Korsmeyer-Peppas release model, from which AZI was released faster compared to raw material.

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Formulation and biopharmaceutical evaluation of bitter taste masking microparticles containing azithromycin loaded in dispersible tablets

Cited by 24 publications

References 46 publications

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

Preparation and Evaluation of Topically Applied Azithromycin Based on Sodium Hyaluronate in Treatment of Conjunctivitis

Evaluation of formulation variables on azithromycin nanoparticles prepared by emulsification solvent diffusion method using quality by design approach

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