Design and Evaluation of Novel Sustained-Release Floating Microspheres for Oral Delivery of Ciprofloxacin Hydrochloride

2021 ◽  
Author(s):  
Parisa Soraya Asa ◽  
Shahla Mirzaeei
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sustained Release ◽  
Oral Administration ◽  
Release Rate ◽  
Diffusion Mechanism ◽  
Oral Dosage ◽  
Mean Particle Size ◽  
The Mean ◽  
Polymer Ratio

Background: Ciprofloxacin (CIP) is a broad-spectrum antibiotic, used to treat various bacterial infections. Administration of conventional oral dosage forms of CIP is associated with multiple challenges such as short residence time of the drug in the gastrointestinal tract which could reduce bioavailability and effectiveness of the drug. This study aimed to design and develop novel floating microspheres for the sustained release of CIP in the stomach over 24 hours after oral administration, besides evaluating the effect of different variables on the characteristics of developed microspheres. Methods: Microspheres were developed by the solvent-evaporation method utilizing cellulose acetate and polyvinyl alcohol, then characterized for physicochemical properties including bulk density, buoyancy, and entrapment efficacy. The drug-excipient compatibility was evaluated by Fourier-transform infrared spectroscopy and the Scanning electron microscopy was used to observe the morphology of microspheres. The effects of the drug to polymer ratio, polymer concentration, and the pace of stirring through the preparation process, on the size and release rate were also evaluated. Results: Morphology analysis indicated round-shape microspheres with a mean particle size between 66-344 µm. The polydispersity index of prepared formulations was determined to be in the range of 0.129 to 0.230. It was observed that at higher polymer concentrations the drug release rate from microspheres decreased while the mean particle size increased. Increasing the drug to polymer ratio and decreasing the stirring speed increased the mean particle size. All formulations showed more than 70% cumulative drug release in the prolonged period of 24 h while remaining buoyant in the meantime. The formulations followed Higuchi and Korsmeyer-Peppas kinetics and release the drug by diffusion mechanism. Conclusions: Based on the results obtained from in vitro release study besides floating properties the prepared microspheres could be considered suitable for enhanced sustained-release of CIP following the oral administration.

scholarly journals Preparation and characterization of Gliclazide incorporated Cellulosic Microspheres: studies on drug release, compatibility and micromeritics

2015 ◽  
Vol 13 (2) ◽  
pp. 149-166 ◽  
Author(s):  
Navid Jubaer Ayon ◽  
Ikramul Hasan ◽  
Md Shfiqul Islam ◽  
Md Selim Reza
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Sustained Release ◽  
Release Rate ◽  
Drug Loading ◽  
Angle Of Repose ◽  
Flow Properties ◽  
Dissolution Apparatus

Polymeric microspheres of gliclazide were prepared to provide sustained release delivery of gliclazide to aid in continuous therapy with high margin of safety. Gliclazide was microencapsulated with different polymers namely HPMC K100LV, Ethocel (20 cps) and HPMC K100M by emulsion solvent evaporation technique using acetone as internal phase and liquid paraffin as external phase. Seventeen formulations were prepared using different drug loading and polymeric ratio of which nine formulations were prepared by a 32 full factorial design. Each formulation was evaluated for flow properties, particle size, surface morphology, drug entrapment efficiency, drug release and compatibility. Yield (%) for every batch of microspheres was measured. Flow properties of the microspheres were examined by determining bulk density, tapped density, Carr’s compressibility index, Hausner ratio and angle of repose. Particle size distribution was examined by sieving and particle size analyzer. Surface morphology was determined by scanning electron microscopy (SEM). In-vitro drug release was studied in a paddle type dissolution apparatus (USP Type II Dissolution Apparatus) for a period of 8 hours at 37°C using phosphate buffer ( pH 7.4). FTIR and DSC studies established compatibility of the drug with the polymers. Microspheres prepared with Ethocel (20 cps) and HPMC K100M were free flowing than those prepared only with HPMC K100LV. Entrapment efficiencies were within 75.88-99.69%. Microspheres prepared with Ethocel (20 cps) and HPMC K100M showed more sustained release when compared to microspheres prepared with HPMC K100LV only. Increase in drug loading resulted in increased drug release for the microspheres. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranging from diffusion controlled to anomalous type. Ethocel and HPMC K100M in a ratio of 1:3 exhibited better sustained release properties than 1:1 and 3:1 ratios. The release rate of gliclazide from microspheres prepared with Ethocel (20 cps) and HPMC K100M was less than the release rate of gliclazide from microspheres prepared with HPMC K100LV, demonstrating Ethocel and HPMC K100M as suitable polymeric blend for preparing the controlled release formulation for gliclazide whereas, HPMC K100LV was found not suitable candidate when used alone as a polymer. DOI: http://dx.doi.org/10.3329/dujps.v13i2.21893 Dhaka Univ. J. Pharm. Sci. 13(2): 149-166, 2014 (December)

scholarly journals FORMULATION AND EVALUATION OF GASTRORETENTIVE MICROBALLOONS OF ACEBROPHYLLINE FOR THE TREATMENT OF BRONCHIAL ASTHMA

2016 ◽  
Vol 9 (5) ◽  
pp. 105
Author(s):  
Subramanian Manivannan ◽  
Akshay M ◽  
Bhuvaneswari S ◽  
Nify F
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Bronchial Asthma ◽  
Residence Time ◽  
Hydroxypropyl Methylcellulose ◽  
Mean Particle Size ◽  
Multiple Unit ◽  
The Mean

ABSTRACTObjective: Gastroretentive dosage forms are an approach for prolonged and predictable drug delivery in the upper gastrointestinal tract to controlthe gastric residence time. Microballoons are considered as one of the most promising buoyant drug delivery systems as they possess the advantagesof both multiple-unit systems and good floating properties. Acebrophylline is a xanthine derivative with potent bronchodilator, mucosecretolytic, andanti-inflammatory property. It is used to treat bronchial asthma and chronic obstructive pulmonary diseases.Methods: Microballoons of acebrophylline were prepared by emulsion solvent diffusion method using hydroxypropyl methylcellulose (HPMC) andethyl cellulose (EC) as polymer. The microballoons were evaluated with their micromeritic properties, particle size, tapped density, compressibilityindex, angle of repose, percentage yield, in vitro buoyancy, entrapment efficiency, drug-polymer compatibility, scanning electron microscopy (SEM),and drug release kinetics.Results: The mean particle size of the microballoons formulation MB1 to MB6 containing HPMC and EC was in the range between 226±16 and 577±10,respectively. The mean particle size of microballoons was found to increase with increasing polymer concentration. The micromeritic properties werefound be good, and SEM confirmed their hollow structure with smooth and dense which helped to prolong floating to increase residence time instomach. The in vitro drug release studies showed controlled release of acebrophylline microballoons in the simulated gastric fluid more than 12 hrs.Conclusions: The results showed that the prepared floating microballoons of acebrophylline prove to be potential multiple-unit delivery devicesadaptable for safe and effective sustained drug delivery.Keywords: Microballoons, Acebrophylline, Bronchial asthma, Hydroxypropyl methylcellulose, Ethyl cellulose.

Development & Pharmaceutical Characterization of Isoniazid Loaded Solid Lipid Nanoparticle Drug Delivery Approach

2019 ◽  
Vol 14 (3) ◽  
pp. 228-238
Author(s):  
Swatantra Kumar Singh Kushwaha ◽  
Awani Kumar Rai ◽  
Heena Parveen
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Sustained Release ◽  
Diffusion Mechanism ◽  
Antitubercular Drug ◽  
Solid Lipid Nanoparticle ◽  
Solid Lipid ◽  
Lipid Nanoparticle

Background: Tuberculosis is a major public health problem in the world. Isoniazid is a first line antitubercular drug active against Mycobacterium species which inhibits mycolic acid synthesis. Objective: The aim of the present investigation was the preparation of solid lipid nanoparticle containing Isoniazid to increase bioavailability, sustained release and decrease toxicity by increasing permeability. Methods: Isoniazid was incorporated into SLN for sustained drug delivery, increasing permeability and bioavailability. SLNs were prepared by emulsification followed by the solvent evaporation technique by optimizing lipid, polymer and surfactant ratio under controlled optimized process variables i.e. temperature and stirring speed. SLNs were characterized for particle size analysis, comparative study design in different physiological pH for in-vitro drug release and drug release kinetics. Results: The best in-vitro release for F7 was found to be 80.2% in pH-7.4 and 82.2% in pH-4.5. The particle size of the F7 formulation was found to be in the range of 200- 600nm . Among all 3 optimized formulations, i.e. F3, F7 and F8 in both the pH, F3 followed non-fickian diffusion mechanism in pH-4.5 whereas all the formulations in both pH followed super-case II diffusion mechanism. The stability studies were carried out as per ICH guidelines which signify that the SLNs were found stable in the refrigerated condition. Conclusion: The results clearly demonstrated that SLNs drug delivery system is a promising approach for antitubercular drug delivery as it proved to sustained release, increase permeability, enhanced bioavailability and thus decreased dosing frequency. Kinetic modelling of the formulation with zero, first order, Higuchi and Korsmeyer- peppas is explained in this article.

Development and Optimization of Inhalable Levofloxacin Nanoparticles for The Treatment of Tuberculosis.

2020 ◽  
Vol 17 ◽  
Author(s):  
Sunny Shah ◽  
Rohit Ghetiya ◽  
Moinuddin Soniwala ◽  
Jayant Chavda
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Factorial Design ◽  
Full Factorial Design ◽  
Pareto Chart ◽  
Mean Particle Size ◽  
Screening Design ◽  
The Mean ◽  
Full Factorial ◽  
32 Full Factorial Design

Background:: Levofloxacin has been recommended by WHO for the treatment of pulmonary tuberculosis and inhalable delivery of levofloxacin can be advantageous over conventional delivery. Objective:: This study aimed to develop and optimize inhalable levofloxacin loaded chitosan nanoparticles (LCN). The objective was to achieve the mean particle size of LCN less than 300nm, sustain the drug release up to 24 h and achieve MMAD of LCN of less than 5μm. Methods:: LCN were prepared by ionic gelation of chitosan with sodium tripolyphosphate (STPP) and subsequent lyophilization. A Plackett Burman screening design, 32 full factorial design, and overlay plot were sequentially employed to optimize the formulation. The mean particle size, % entrapment efficiency, in vitro drug release, and Minimum inhibitory concentration were evaluated. Results:: The Pareto chart from Placket Burman screening design revealed that the concentration of chitosan and concentration of STPP were found to be significant (p < 0.05). Further analysis by 32 full factorial design revealed that F-ratio for each model generated was found to be greater than the theoretical value (p < 0.05), confirming the significance of each model. Conclusion:: The optimized formulation showed a mean particle size of 171.5 nm, sustained the drug release up to 24 h in simulated lung fluid, and revealed MMAD of 3.18 μm, which can confirm delivery of the drug to deep lung region. However, further in vivo studies are required to design suitable dosage regimen and establish the fate of nanoparticles for safe and efficacious delivery of the drug.

scholarly journals Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 260 ◽  
Author(s):  
Dongwei Wan ◽  
Min Zhao ◽  
Jingjing Zhang ◽  
Libiao Luan
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Diffusion Rate ◽  
Immediate Release ◽  
Pharmacokinetic Studies ◽  
Release Tablet

This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo.

Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

2020 ◽  
pp. 1-9
Author(s):  
Yunhong Wang ◽  
Rong Hu ◽  
Yanlei Guo ◽  
Weihan Qin ◽  
Xiaomei Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Orthogonal Design ◽  
Drug Loading ◽  
In Vitro Release ◽  
Core Material ◽  
Evaluation Indexes ◽  
Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

Amoxicillin-loaded polyethylcyanoacrylate nanoparticles: Influence of PEG coating on the particle size, drug release rate and phagocytic uptake

Biomaterials ◽  
2001 ◽  
Vol 22 (21) ◽  
pp. 2857-2865 ◽  
Author(s):  
Giacomo Fontana ◽  
Mariano Licciardi ◽  
Silvana Mansueto ◽  
Domenico Schillaci ◽  
Gaetano Giammona
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Rate ◽  
Drug Release Rate ◽  
Peg Coating ◽  
Phagocytic Uptake

scholarly journals Formulation and characterization of flurbiprofen loaded microsponge based gel for sustained drug delivery

2019 ◽  
Vol 10 (4) ◽  
pp. 2765-2776
Author(s):  
Naresh Kshirasagar ◽  
Goverdhan Puchchakayala ◽  
Balamurgan K
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Diffusion Method ◽  
Skin Delivery ◽  
Sustained Action ◽  
Release Studies ◽  
Ft Ir ◽  
Polymer Ratio

The new investigation in this present work is to develop microsponges constructed novel drug delivery system for sustained action of Flurbiprofen. Quai-emulsion solvent diffusion method was engaged using Ethyl cellulose and Eudragit RS100 with drug: polymer ratio for development of microsponges. For optimization purposes, several factors are considered in the investigation. Several evaluation studies for the formed microsponges were carried out FT-IR, SEM, DSC, X-RD, particle size analysis, morphology, drug loading and In vitro drug release studies were carried out. Finally, it was concluded that there is no drug-polymer interaction as per DSC & FT-IR. Encapsulation efficiency, particle size and drug content showed a higher impact on alteration of drug-polymer ratio. SEM studies showed that morphological microsponges are spherical and porous in nature and with the mean particle size of 38.86 μm. The gel loaded with microsponges, were followed by In vitro and Ex vivo drug release studies by modified Franz diffusion cell. Skin delivery of optimized formulation enhanced the drug residence time and maintained therapeutic concentration for an extended period of time, which is possible to show sustained action of the drug.

Effect of Ag addition in Sn on growth of SnTe compound during reaction between molten solder and tellurium

2010 ◽  
Vol 25 (2) ◽  
pp. 391-395 ◽  
Author(s):  
Chien-Neng Liao ◽  
Yen-Chun Huang
Keyword(s):  
Particle Size ◽  
Reaction Time ◽  
Electrical Properties ◽  
Bismuth Telluride ◽  
Molten Solder ◽  
Thermoelectric Modules ◽  
Ag Addition ◽  
Mean Particle Size ◽  
Mechanical And Electrical Properties ◽  
The Mean

SnTe is the most common compound formed at the bismuth telluride/metal soldered junction of thermoelectric modules. It affects the mechanical and electrical properties of the soldered junction. In the study we investigate the growth of SnTe compound during reaction between molten Sn–3.5Ag solder and tellurium at 250 °C. We found that the growth of SnTe is suppressed by Ag–Te bilayer compounds that block further reaction between liquid Sn and Te. With increasing reaction time, the SnTe morphology becomes rough as a result of coarsening of SnTe grains. The growth of SnTe grains follows the conservative ripening kinetics with the mean particle size proportional to one-third power of reaction time.

Microstructure and Thermodynamic Analysis of Graphene-Reinforced Coating Surface

2021 ◽  
Vol 1033 ◽  
pp. 56-60
Author(s):  
He Ping Liu ◽  
Heng Zhe Yang ◽  
Lang Lang Liu ◽  
Feng Er Sun ◽  
Xiao Min Yang ◽  
...  
Keyword(s):  
Particle Size ◽  
Thermodynamic Analysis ◽  
Induction Coil ◽  
Mean Particle Size ◽  
Substrate Distance ◽  
Cladding Layer ◽  
Coating Surface ◽  
The Mean ◽  
Graphene Content

The microstructure of coatings with different graphene content and the hardness of cladding layer under different distance between coil and samples were investigated. The results showed that with the increase of graphene, the mean particle size of the powder did not get significantly coarser. The defects and oxides were appeared in the cladding layer and graphene diffused into the substrate. Distance between induction coil and sample has great impact on the hardness of coating, the higher hardness was measured in the distance between 6-8cm. The thermodynamic analysis of coating nucleation was carried out.

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