Floating ability and drug release evaluation of gastroretentive microparticles system containing metronidazole obtained by spray drying

Abstract

Gastroretentive floating microparticles were developed and evaluated for the controlled metronidazole delivery for treatment of gastric disease. Floating microparticles, varying in proportions of chitosan and hydroxypropyl methylcellulose or ethylcellulose, were obtained by spray drying. Floating microparticles were characterized by physicochemical and in vitro studies, according to their floating ability and drug delivery. Microparticles presented mean diameter from 1.05 to 2.20 µm. The infrared spectroscopy confirmed the drug encapsulation and showed no chemical linkage between microparticles components. X-ray diffraction showed changes in the drug`s solid state, from crystalline to amorphous, indicating partial drug encapsulation, due to the presence of some crystalline peaks of metronidazole in microparticles. All microparticles floated immediately in contact of simulated gastric fluid and both floating and drug release profiles were dependent of microparticles composition. Microparticles samples constituted by chitosan and hydroxypropyl methylcellulose revealed the best relationship between floating duration and drug release, remaining floating during the occurrence of the drug release, ideal condition for the floating gastroretentive systems.Uniterms: Floating microparticle. Chitosan. Ethylcellulose. Hydroxypropyl methylcellulose. Controlled drug delivery.

Developed meloxicam loaded microparticles for colon targeted delivery: Statistical optimization, physicochemical characterization, and in-vivo toxicity study

“…The XRD pattern of pure MLX demonstrates individual intense peaks between the range of 6–30˚ at 2θ of diffraction angle corresponding to 13.17˚, 15.06˚, 18.49˚, and 26.07˚, which demonstrates the crystalline nature of MLX, as shown in Fig 7(A) [ 38 , 70 ]. The HPMC illustrated a wide hump in between the range of 5˚-25˚, which reflects its amorphous state, as displayed in Fig 7(B) [ 74 ]. The XRD pattern of the physical mixture of the MLX as well as HPMC, and optimized formulation (F0) maintained their peaks, which revealed that there was no interaction between the ingredients of the physical mixture and optimized formulation, as depicted in Fig 7(C) and 7(D) [ 75 ].…”

Clinical comparative study of optimized metronidazole loaded lipid nanocarrier vaginal emulgel for management of bacterial vaginosis and its recurrence

“…The prepared MTD-SLNs dispersions were centrifuged using a cooling centrifuge (2-16KL, Sigma Laborzentrifugen GmbH, Osterode am Harz, Germany) at 12,000 rpm for 2 h at 4 °C (Badawi et al., 2018 ). The supernatant was collected to measure the free drug concentration using ultraviolet (UV) spectrophotometer (V-630, Jasco, Tokyo, Japan) at 277 nm (Nohemann et al., 2017 ). The entrapment efficiency percent EE% was calculated according to the following equation (Badawi et al., 2018 ): …”

“…The precise volume of the samples was withdrawn at regular time intervals till 24 h and replaced with an equal volume of fresh dissolution media. The cumulative release of MTD from lipid nanoparticles was determined spectrophotometrically at 277 nm (Nohemann et al., 2017 ).…”

“…Following a 1 ml of 50 ml volumetric flask was diluted in a 10 ml volumetric flask. The amount of drug for each one gram gel was detected spectrophotometrically at 277 nm (Nohemann et al., 2017 ) and the drug content was calculated using the calibration curve (Wang et al., 2012 ).…”

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“…Metronidazole is an antibiotic, amebicide, and antiprotozoal used particularly for anaerobic bacteria and protozoa. The unionized metronidazole having the ability to reduce intercellularly, this reduced form covalently binds to DNA, disrupt its helical structure, inhibiting bacterial nucleic acid synthesis and resulting in bacterial cell death 11,12 . Metronidazole widely used for the treatment of H. Pylori eradication therapy, in combination with other antibiotics and one proton pump inhibitor.…”