Floating microspheres of Miglitol as gastro retentive drug delivery system: 32 full factorial design and in vitro evaluation

Abstract Background: The goal of this study was to develop a gastro retentive floating drug delivery system that would improve site specific activity, patient compliance and therapeutic efficacy.Methodology: Floating microspheres of Miglitol were formulated by double emulsion method using ethyl cellulose and eudragit E100 different weight ratio and PVA as an emulsifier. It has been prepared with respect quantity of polymer concentration and stirring speed to evaluate for % buoyancy, drug entrapment efficiency, particle size drug release rate. Result: The percent of buoyancy, drug entrapment efficiency, particle size, and percentage yield were increased with increase the polymer mixture concentration. Among all formulation batches, F6 showed acceptable results drug entrapment efficiency (86.57%) and buoyancy (94.25%). F10 formulation was prepared to check the predicted and actual factors and compared with optimized formulation F6. The drug release was increased as the polymer concentration was decrease. The kinetic model zero order had the highest regression coefficient value, it was described as a sustained release dosage form. According to ICH guideline accelerated stability studies of F6 and F10 formulations were conducted for 90 days. After 90 days buoyancy and in vitro drug release was performed and the results were F6 and F10 buoyancy was found to be 88.21%, 87.22% and in vitro drug release was found to be 62.87%, 63.51%. Conclusion: The present study, showed compatibility of drug with polymers by FTIR in formulation. Floating microsphere of Miglitol was prepared by double emulsion technique. The F6 Miglitol floating microsphere was optimized formulation demonstrated with excellent drug entrapment performance (86.57%), good floating behaviour (94.25%), and the largest particle size (670µm). The present study concludes that floating based gastro retentive delivery system of Miglitol microspheres has a safe and effective drug delivery system with increased therapeutic efficacy and a longer duration of action.

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Floating Microsphere of Curcumin as Targeted Gastro-retentive Drug Delivery System

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.00905 ◽

2021 ◽

pp. 5202-5206

Author(s):

Anupam K Sachan ◽

Saurabh Singh ◽

Kiran Kumari ◽

Pratibha Devi

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Sustained Release ◽

Drug Delivery System ◽

Delivery System ◽

Entrapment Efficiency ◽

Synthetic Polymers ◽

Drug Bioavailability ◽

Gastric Residence Time

Microspheres carrier system made from natural or synthetic polymers used in sustained release drug delivery system. The present study involves formulation and evaluation of floating microspheres of Curcumin for improving the drug bioavailability by prolongation gastric residence time. Curcumin, natural hypoglycemic agent is a lipophilic drug, absorbed poorly from the stomach, quickly eliminated and having short half-life so suitable to formulate floating drug delivery system for sustained release. Floating microspheres of curcumin were formulated by solvent evaporation technique using ethanol and dichloromethane (1:1) as organic solvent and incorporating various synthetic polymers as coating polymer, sustain release polymers and floating agent. The final formulation were evaluated various parameters such as compatibility studies, micrometric properties, In-vitro drug release and % buoyancy. FTIR studies showed that there were no interaction between drug and excipients. The surface morphology studies by SEM confirmed their spherical and smooth surface. The mean particles size were found to be 416-618µm, practical yield of microspheres was in the range of 60.21±0.052% - 80.87±0.043%, drug entrapment efficiency 47.4±0.065% - 77.9±0.036% and % buoyancy 62,24±0.161% - 88.63±0.413%. Result show that entraptmency increased as polymer (Eudragit RS100) conc. Increased. The drug release after 12 hrs. was 72.13% - 87.13% and it decrease as a polymer (HPMC, EC) concentration was decrease.

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Development and In-Vitro Evaluation of Budesonide Mucoadhesive Microspherefor Pulmonary Drug Delivery

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v11i2-s.4622 ◽

2021 ◽

Vol 11 (2-S) ◽

pp. 76-81

Author(s):

Jddtadmin Journal

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Drug Release ◽

Chemical Interaction ◽

Entrapment Efficiency ◽

Pulmonary Drug Delivery ◽

Sustained Drug Release ◽

In Vitro Drug Release ◽

Drug Entrapment Efficiency

Thepurpose of the study was to develop and evaluatemucoadhesive microspheres of Budesonide for pulmonary drug delivery systemhaving prolonged residence time and sustained drug release. Microspheres were prepared by emulsificationsolvent evaporation technique using HPMC, carbopol as polymers in varying ratios. The microspheres were evaluated for its percentage yield, drug entrapment efficiency, particle size and shape, in vitro mucoadhesion study and in vitro drug release studies.The FTIR studies revealed no chemical interaction between the drug molecule and polymers and found that drug was compatible with used polymer. The mucoadhesive microspheres showed particle size, drug entrapment efficiency and yield in the ranges of148 - 164 μm, 68.0 - 85.0%and67.52 - 87.25% respectively. In vitro drug release and mucoadhesion study confirms thatformulationF5 was the best formulation as it releases 81.8 % at the end of 12 hr. in controlled manner and percentage mucoadhesion of 75.2 % after 10 hr. This confirms the developed budesonidemucoadhesive microspheres are promising for pulmonary drug delivery system. Keywords: Budesonide, Mucoadhesion, Microspheres, Drug entrapment efficiency.

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DEVELOPMENT AND IN VITRO EVALUATION OF FLOATING DRUG DELIVERY SYSTEM OF ACECLOFENAC

INDIAN DRUGS ◽

10.53879/id.53.09.10548 ◽

2016 ◽

Vol 53 (09) ◽

pp. 63-66

Author(s):

J. C Rathi ◽

◽

V. Rathi ◽

S. Tamizharasi

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Entrapment Efficiency ◽

Gastric Residence Time ◽

Floating Drug Delivery ◽

Drug Entrapment Efficiency ◽

Floating Drug Delivery System ◽

Central Composite

The objective of the present investigation is to attain optimized floating drug delivery system for aceclofenac by determining the effects of some important factors for the prolongation of gastric residence time. Floating microspheres were prepared by solvent diffusion–evaporation method using ethyl cellulose and hydroxypropylmethylcellulose. A central composite design was applied to optimize the formulation. An appropriate balance between the levels of the polymer and stirring speed was imperative to acquire maximum drug entrapment efficiency, sustained release of the drug, floating ability and adequate particle size.

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Development, Characterization, and In Vitro Evaluation of Resveratrol-Loaded Poly-(ε-caprolactone) Microcapsules Prepared by Ultrasonic Atomization for Intra-Articular Administration

Pharmaceutics ◽

10.3390/pharmaceutics11060249 ◽

2019 ◽

Vol 11 (6) ◽

pp. 249 ◽

Cited By ~ 4

Author(s):

Asteria Luzardo-Álvarez ◽

Iván Lamela-Gómez ◽

Francisco Otero-Espinar ◽

José Blanco-Méndez

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Drug Delivery System ◽

Delivery System ◽

Inflammatory Responses ◽

Polymer Concentration ◽

Joint Disease ◽

Oral Drug ◽

Ultrasonic Atomization

Intra-articular administration of drugs to the joint in the treatment of joint disease has the potential to minimize the systemic bioavailability and the usual side-effects associated with oral drug administration. In this work, a drug delivery system is proposed to achieve an anti-inflammatory local effect using resveratrol (RSV). This study aims to develop microcapsules made of poly-(ε-caprolactone) (PCL) by ultrasonic atomization to preserve the antioxidant activity of RSV, to prevent its degradation and to suppress the inflammatory response in activated RAW 264.7 macrophages. An experimental design was performed to build a mathematical model that could estimate the effect of nozzle power and polymer concentration on particle size and encapsulation efficiency. RSV-loaded microcapsules showed adequate morphology, particle size, and loading efficiency properties. RSV formulations exhibited negligible cytotoxicity and an efficient amelioration of inflammatory responses, in terms of Nitric Oxide (NO), ROS (Reactive Oxygen Species), and lipid peroxidation in macrophages. Thus, RSV-loaded microcapsules merit consideration as a drug delivery system suitable for intra-articular administration in inflammatory disorders affecting the joint.

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Physico-chemical evaluation of Gastroretentive Ranitidine Hydrochloride: An Anti-Ulcer Drug

Janaki Medical College Journal of Medical Science ◽

10.3126/jmcjms.v3i2.16075 ◽

2016 ◽

Vol 3 (2) ◽

pp. 4-12

Author(s):

RK Yadav ◽

Satyam Prakash ◽

K Yadav ◽

NK Yadav ◽

M Mostafa

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Entrapment Efficiency ◽

Lag Time ◽

Gastric Fluid ◽

Simulated Gastric Fluid ◽

Drug Content ◽

Drug Entrapment Efficiency ◽

Gastro Retentive

Background and Objectives: The prevention and treatment of peptic ulcers has become an important challenge in the current medicine world. Modern progress in novel drug delivery system aims to improve the efficacy of the drug molecule by formulating a dosage form of RHCL. One of the most feasible approaches for achieving a prolonged and predictable drug delivery profile in GI tract is to control the gastric residence time. Therefore, a multi-unit gastro retentive dosage form of RHCL capable of floating on simulated gastric fluid for more than 12 hours was formulated and evaluated.Materials and Methods: Nine batches of the light liquid paraffin entrapped emulsion gel beads were prepared by a new emulsion gelation technique using sodium alginate and xanthan gum as polymers. The polymeric solution was extruded into Calcium chloride solution by the use of 21G needles. Morphology of beads, drug content, drug entrapment efficiency, floating lag time and buoyancy were studied. Compatibility study of Ranitidine HCl with polymers used in the formulation was performed using DSC and FT-IR.Results: Mean surface diameter were between 1.220 ± 2.259% (F1) to 1.230 ± 2.316% (F9) and floating lag time were between 6 minute (F9) to 11 minute (F1). All formulations were buoyant for more than 12 hours in simulated gastric fluid at 37ºC. The drug content and drug entrapment efficiency among the formulations were between 17.48%~19.68% and 71.06% ~84.32% respectively. Formulation F1 showed lowest drug content and drug entrapment efficiency while F9 showed highest drug content and drug entrapment efficiency. F4 showed most acceptable sustained drug release profile.Conclusion: The gastro retentive drug delivery system designed as floating beads was found to be satisfactory drug delivery system for Ranitidine HCl to improve the bioavailability of the drug. Janaki Medical College Journal of Medical Sciences (2015) Vol. 3 (2): 4-12

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PREPARATION, CHARACTERIZATION AND STABILITY STUDIES OF SOLID SELF EMULSIFYING DRUG DELIVERY SYSTEM OF NIFEDIPINE

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2020v12i2.36406 ◽

2020 ◽

pp. 94-102

Author(s):

SABITRI BINDHANI ◽

SNEHAMAYEE MOHAPATRA ◽

RAJAT KUMAR KAR

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Drug Release ◽

Dissolution Rate ◽

Drug Delivery System ◽

Delivery System ◽

Linseed Oil ◽

Stability Study ◽

In Vitro Dissolution

Objective: The objective of this work was to improve the solubility and dissolution rate of Nifedipine by preparing a solid-self micro emulsifying drug delivery system (Solid-smedds). Methods: Liquid-self-emulsifying drug delivery system formulations were prepared by using linseed oil as oil, tween 80 as a surfactant and PEG 400 as cosurfactant. Components were selected by solubility screening studies and the self-emulsifying region was identified by the pseudo-ternary phase diagram. Thermodynamic stability study was performed for the determination of stable liquid-smedds formulation. These formulations were evaluated for self-emulsification time, drug content analysis, robustness to dilution test, particle size analysis, in vitro diffusion study, and Stability study. Solid self-micro emulsifying formulations were prepared by using aerosil-200 at a different ratio. Lf9S (0.65:1) was selected due to its highest drug entrapment efficiency and a decrease in particle size. It was selected for further studies into DSC, SEM, FTIR, and XRD analysis. Results: DSC and XRD result shows that the drug within the formulation was in the amorphous state. From the SEM study, it was observed that the drug has been uniformly distributed and having a smooth surface. From the in vitro dissolution study, it improved the dissolution rate of nifedipine which was 98.70% of drug release where pure drug release only 6.72%. Conclusion: In conclusion, a solid self-micro emulsifying drug delivery system is improved the solubility and drug release rate but also improved the stability of the formulation.

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Enhancement of Nimodipine Solubility by Self-Nano-emulsifying Drug Delivery System

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2019.12.5.5 ◽

2019 ◽

Vol 12 (5) ◽

pp. 4648-4656

Author(s):

Suresh Gande ◽

S. Srikanth Reddy ◽

Bhikshapathi D. V. R. N.

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

Drug Delivery System ◽

Delivery System ◽

Spherical Shape ◽

Drug Dissolution ◽

The Stability

Self-nanoemulsifying drug delivery system (SNEDDS) of Nimodipine was developed with the purpose of improving the bioavailability of the drug. Based on the results of Nimodipine solubility studies Peceol, Transcutol P and PEG 400 were optimized as oil, surfactant and co-surfactant for the formulation and Pseudo ternary plots was constructed by Chemix software. Fifteen formulations of Nimodipine SNEDDS prepared and analyzed for particle size, emulsification time, percentage drug release, percentage transmittance, in vitro drug dissolution studies and thermodynamic stability. The optimized Nimodipine SNEDDS formulation (F13) subjected to drug-excipient compatibility studies by FTIR. They are analyzed for zeta potential, SEM and stability. The particle size of optimized Nimodipine SNEDDS formulation was 25.9 nm, PDI is 0.382 and zeta potential -12.7 mV that are optimal for the stability of emulsion. SEM studies of Nimodipine SNEDDS indicated spherical shape and uniform particle distribution. The drug release of formulation F13 (98.25±4.77%) was higher than pure drug (38.49±3.88%). The stability studies indicated no change in drug content, drug release, emulsifying properties and appearance. Hence a potential SNEDDS formulation of Nimodipine developed with increased dissolution rate, bioavailability and solubility.

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SUSTAINED RELEASE MULTIPARTICULATE GASTRORETENTIVE DELIVERY SYSTEM OF CINNARIZINE

INDIAN DRUGS ◽

10.53879/id.51.07.10109 ◽

2014 ◽

Vol 51 (07) ◽

pp. 31-38

Author(s):

Gurudev Kruthi ◽

◽

B. V. Basavaraj ◽

S. Bharath ◽

R. Deveswaran ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Delivery System ◽

Polymer Concentration ◽

Entrapment Efficiency ◽

Ir Studies ◽

Sustained Drug Delivery ◽

Release Studies ◽

Drug Entrapment Efficiency

The main aim of the present work was to formulate and evaluate sustained release multiparticulate gastroretentive delivery system of cinnarizine. The microspheres were prepared by solvent evaporation method by using Eudragit RS 100 as a polymer in varying ratios. The prepared microspheres were evaluated for drug – polymer compatibility studies, micromeritic properties, drug entrapment efficiency, in vitro buoyancy and drug release studies. The mean particle size increased with increase in polymer concentration, ranging between 60.33 μm to 144.88 μm. FT IR studies showed that the drug and polymer were compatible with each other. The entrapment efficiency decreased with increase in the polymer concentration with values of 50%, 33.3% and 25% respectively. The microspheres floated upto 9 h over the surface of the gastric buffer medium and the buoyancy percentage was found to be in the range of 64.3 – 76.2%. In vitro drug release studies showed that the prepared microspheres exhibited prolonged drug release upto 62.89% for more than 9 h. The mechanism of drug release was found to be a combination of both peppas and matrix kinetics. Thus the developed floating microspheres of cinnarizine may be used as sustained drug delivery system for increasing the therapeutic efficacy with an improved patient compliance.

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FORMULATION, CHARACTERIZATION AND IN VITRO EVALUTION OF GABAPENTIN FLOATING MICROSPHERES

INDIAN DRUGS ◽

10.53879/id.54.01.10598 ◽

2017 ◽

Vol 54 (01) ◽

pp. 20-27

Author(s):

H. B Samal ◽

I. J. Das ◽

P. N. Murthy ◽

Keyword(s):

Particle Size ◽

Drug Release ◽

Release Kinetics ◽

Polymer Concentration ◽

Average Particle Size ◽

Entrapment Efficiency ◽

Linear Regression Method ◽

Average Particle ◽

Drug Entrapment Efficiency

The present study involves the design and characterization of floating microspheres with gabapentin as model drug for prolongation of gastric residence time. Gabapentin floating microspheres were prepared by o/w/o emulsification solvent diffusion technique using ethyl cellulose as the rate controlling polymer at various concentrations. The shape and surface morphology of microspheres were characterized by optical and scanning electron microscopy. Absence of drug-polymer interaction was confirmed by FTIR analysis. In vitro drug release studies were performed and drug release kinetics was evaluated using the linear regression method. Effects of polymer concentration, solvent composition, particle size, drug entrapment efficiency and drug release were also studied. The synthesized microspheres exhibited prolonged drug release (> 12 h) and remained buoyant for > 24 h. The drug entrapment efficiency was in the range 46-70 %. At higher polymer concentration, the average particle size was increased and the drug release rate decreased. In vitro studies revealed diffusion-controlled drug release from the microspheres. Among all the formulations (F1-F5), F4 is the optimized formulation.

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DEVELOPMENT OF GASTRO-RETENTIVE FLOATING MICROSPHERES OF ONDANSETRON HYDROCHLORIDE

INDIAN DRUGS ◽

10.53879/id.51.08.10142 ◽

2014 ◽

Vol 51 (08) ◽

pp. 22-27

Author(s):

S. G Bandbe ◽

◽

K Dixit ◽

G Laghate ◽

R. B. Athawale

Keyword(s):

Particle Size ◽

Drug Release ◽

Ethyl Cellulose ◽

Polymer Concentration ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Ondansetron Hydrochloride ◽

Percentage Yield ◽

Gastro Retentive

Ondansetron hydrochloride (OND) is indicated for prevention of nausea and vomiting during chemotherapy. Due to its insolubility in intestinal pH, it is absorbed only in the stomach. In the present study, an attempt was made to increase gastric retention time of ondansetron hydrochloride by preparing its floating microspheres by solvent evaporation method with ethyl cellulose (EC) and hydroxypropylmethylcellulose (HPMC). Microspheres were characterized for percentage yield, particle size, surface morphology, floating behaviour, entrapment efficiency and in vitro release. Polymer ratio and stirring speed seemed to have significant impact on size, entrapment efficiency, floating time and release profile. Hydroxypropylmethylcellulose: ethyl cellulose in the ratio 1: 3, gave most suitable buoyancy and drug release. By increasing polymer concentration, the mean particle size of microspheres increased while drug release rate decreased. Developed formulation of ondansetron hydrochloride can be used for prolonging its retention in the stomach for at least 12 hrs, thereby improving bioavailability and patient compliance.

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