Formulation and In vitro Evaluation of Floating Microspheres of Misoprostol

2017 ◽  
Vol 10 (1) ◽  
pp. 3608-3615
Author(s):  
K Vanitha ◽  
M. Mohan Varma ◽  
Ramesh Alluri
Keyword(s):  
Drug Release ◽  
High Performance ◽  
Chemical Interaction ◽  
Release Kinetics ◽  
Diffusion Mechanism ◽  
Methyl Cellulose ◽  
Ultra Violet ◽  
Fickian Diffusion ◽  
Polymer Ratio

Misoprostol is a synthetic prostaglandin PGE1 analogue, which has proved to be an effective anti-secretory agent for oral use. The major indications of Misoprostol are in the prevention and treatment of NSAID-induced gastric and duodenal ulcers. Its half-life is 20-40 minutes. More than one third of patients with ulcers are resistant to H2 antagonists. So, these patients can be healed on Misoprostol. The objective of the present study was to formulate gastroretentive floating drug delivery system of an antiulcer drug Misoprostol. Floating microspheres of Misoprostol were prepared by an emulsification solvent evaporation technique using hydroxy propyl methyl-cellulose (HPMC K 100M) and ethyl cellulose. The percentage yield and drug entrapment efficiencies of these floating microspheres were within the range between: 70 ± 2.8 to 98 ± 2.9 % and 39.27 to 82.39 %, respectively. The determined mean particle size for all the microspheres were 250 ± 7.28 to 400 ± 2.32 µm. The flowability of these microspheres was found good. A high performance liquid chromatography (HPLC) method with ultra-violet (UV) detection was selected for the method of analysis.  The drug release was found to delay for 12 hours with the increasing drug to polymer ratio. The drug release kinetics followed Korsemeyer-Peppas and Higuchi model with anomalous (non-Fickian) diffusion mechanism for the drug release. The FTIR and DSC studies showed that there was an absence of chemical interaction between the drug and the excipients. The in vitro drug release from Misoprostol floating microspheres showed the drug release was dependent on the drug to polymer ratio. The drug release was found delayed with the increasing drug to polymer ratio.  

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

Design and Synthesis of a Novel Gabapentin-Phosphotidylcholine Conjugate for Targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier

2020 ◽  
Vol 16 ◽  
Author(s):  
Anjali P.B ◽  
Jawahar N. ◽  
Jubie S. ◽  
Neetu Yadav ◽  
Selvaraj A. ◽  
...  
Keyword(s):  
Drug Release ◽  
Phospholipase A2 ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Structural Analog ◽  
Fickian Diffusion ◽  
Release Kinetic ◽  
Nanostructured Lipid Carrier ◽  
Discovery Studio

Background: : Epilepsy is a genuine neurological turmoil that effects around 50 million individuals around the world. Practically 30% of epileptic patients experience the ill effects of pharmaco-obstruction, which is related with social seclusion, subordinate conduct, low marriage rates, joblessness, mental issues and diminished personal satisfaction. At present accessible antiepileptic drugs have a restricted viability, and their negative properties limit their utilization and cause challenges in patient administration. Gabapentin 1-(aminomethyl)cyclohexane acetic acid, Gbp , (trade name Neurontin), a structural analog of γ-aminobutyric acid (GABA), BCS class 3 drug with having permeability issues. Objective: This work was an attempt to formulate and characterize a new approach to treat epilepsy by targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier. Methods: Docking studied carried out using Accelrys Discovery studio 4.1 Client and gabapentin and phosphotidylcholine were conjugated through chemical conjugation. Nanostructured lipid carrier (NLC) was prepared using hot homogenization technique. Results: The libdock score of Gabapentin- Phosphotidylcholine conjugate (192.535) were found to be more than Gabapentin (77.1084) and Phosphotidylcholine (150.212). For the optimized formulation the particle size (50.08), zeta potential (-1.48), PDI (0.472) and entrapment efficiency (77.8) was observed. The NLC was studies for in-vitro drug release studies and release kinetics. Finally found that the drug release from the NLC followed Higuchi release kinetic and the mode of drug release from the NLC was found to be Non- Fickian diffusion. Conclusion: The formulated Nanostructured lipid carrier of Gabapentin-Phosphotidylcholine conjugate may be able to use to prevent seizure.

scholarly journals Polymer/Iron-Based Layered Double Hydroxides as Multifunctional Wound Dressings

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1130
Author(s):  
Mariana Pires Figueiredo ◽  
Ana Borrego-Sánchez ◽  
Fátima García-Villén ◽  
Dalila Miele ◽  
Silvia Rossi ◽  
...  
Keyword(s):  
Drug Release ◽  
High Performance ◽  
Mechanical Performance ◽  
Release Kinetics ◽  
Wound Dressings ◽  
In Vitro Drug Release ◽  
Improved Performance ◽  
Double Hydroxide ◽  
Double Hydroxides

This work presents the development of multifunctional therapeutic membranes based on a high-performance block copolymer scaffold formed by polyether (PE) and polyamide (PA) units (known as PEBA) and layered double hydroxide (LDH) biomaterials, with the aim to study their uses as wound dressings. Two LDH layer compositions were employed containing Mg2+ or Zn2+, Fe3+ and Al3+ cations, intercalated with chloride anions, abbreviated as Mg-Cl or Zn-Cl, or intercalated with naproxenate (NAP) anions, abbreviated as Mg-NAP or Zn-NAP. Membranes were structurally and physically characterized, and the in vitro drug release kinetics and cytotoxicity assessed. PEBA-loading NaNAP salt particles were also prepared for comparison. Intercalated NAP anions improved LDH–polymer interaction, resulting in membranes with greater mechanical performance compared to the polymer only or to the membranes containing the Cl-LDHs. Drug release (in saline solution) was sustained for at least 8 h for all samples and release kinetics could be modulated: a slower, an intermediate and a faster NAP release were observed from membranes containing Zn-NAP, NaNAP and Mg-NAP particles, respectively. In general, cell viability was higher in the presence of Mg-LDH and the membranes presented improved performance in comparison with the powdered samples. PEBA containing Mg-NAP sample stood out among all membranes in all the evaluated aspects, thus being considered a great candidate for application as multifunctional therapeutic dressings.

scholarly journals Design and Characterization of Combinational Domperidone-Famotidine Floating Drug Delivery System - In vitro and In vivo studies

2021 ◽  
Vol 62 (2) ◽  
pp. 144-162
Author(s):  
Mounika Chidurala ◽  
Raveendra Reddy J
Keyword(s):  
Drug Release ◽  
Oral Administration ◽  
Quality By Design ◽  
Release Kinetics ◽  
Cost Effective ◽  
Fickian Diffusion ◽  
In Vivo Studies ◽  
Pharmacokinetic Studies

Introduction: The drawbacks assosiated with oral administration of drugscan be controlled or minimized by gastro retentive formulations that remain buoyant within the stomach for an extended time by providing prolonged gastric retention and releasethe drug in an exceedingly extended manner thereby improving bioavailability. The current research was to develop and optimize Domperidone and Famotidine floating tablets with extended release by Quality by Design approach. Method: Based on QTPP (Quality Target Product Profile), CQAs (Critical Quality Attributes)wereidentified. Risk analysis by the evaluation of formulation and process parameters showed that optimizing the levels of polymers could reduce high risk to achieve the target profile. A 23factor experimental design with midpoints was selected for statistical analysis and optimization. Results: HPMC K100 and Carbopol 934P had a positive effect while ethyl cellulose demonstrated a negative effect on the selected responses. Drug release kinetics followed the first-order release with Higuchi diffusion and Fickian diffusion. Optimized formula satisfying all the required parameters was selected and evaluated. The predicted response values were in close agreement with experimental response values. Abdominal X-ray imaging after oral administration of the tablets on a healthy rabbit’s stomach confirmed the extended floating behavior with shorter lag time. In vivo, pharmacokinetic studies in rabbits revealed that the optimized formulation exhibited prolonged drug release with enhanced Cmax, tmax, AUCo-t, and t1/2 of an optimized product when compared to the marketed product. Conclusions: It has been concluded that the application of Quality by Design in the formulation and optimization reduced the number of trials to produce a cost-effective formula.

Quality by Design enabled anti-hypertensive Floating drug delivery system by Risk assessment and Design of Experiment (DoE) – In vitro – In vivo correlation studies

2021 ◽  
Vol 16 ◽  
Author(s):  
Mounika Chidurala ◽  
Raveendra Reddy J
Keyword(s):  
Drug Release ◽  
Risk Analysis ◽  
Quality By Design ◽  
Release Kinetics ◽  
Cost Effective ◽  
Fickian Diffusion ◽  
In Vivo Studies ◽  
Pharmacokinetic Studies

Background: The present research aimed to develop and optimize extended-release floating tablets of Sacubitril and Valsartan through Quality by Design (QbD) approach. Risk analysis by formulation assessment and process parameters showed that optimizing the levels of the polymer will minimize high risk to meet the target profile. A two (2) level three (3) full factorial experimental design along with midpoints was carefully chosen for optimization and statistical analysis. Based on the literature, the independent and dependent variables were selected. Results: HPMC K100, Carbopol 934P had a positive effect, whereas Ethylcellulose had a negative effect on Floating time, drug release at 2 h, drug release at 12 h and, 50% responses. Drug release kinetics followed the first-order release with Higuchi and Fickian diffusion. Contour and overlay plots were utilized for an assortment of design space and optimized formula. ANOVA results of all the factors exhibited significance at p<0.05. Abdominal X-ray imaging of the optimized tablets on healthy rabbit’s stomach confirmed the floating behavior for more than 12 h. In vivo pharmacokinetic studies in rabbits showed that the optimized formulation exhibited prolonged and extended drug release with improved Cmax, tmax, AUCo-t, and t1/2 of test product when compared to marketed product. IVIVC model was developed by using dissolution data of in vitro and pharmacokinetics data of in-vivo by de-convolution method (Wagner-Nelson method). Conclusion: The Quality by Design implementation in the formulation and optimization abridged the number of trials to produce a cost-effective formula. In vivo studies confirmed that the formula was successfully developed with extended floating time (12 h) and drug release by risk analysis and experimental designs. Level A correlation was observed which confirmed a good correlation between in vitro and in vivo data.

scholarly journals PREPARATION, PHYSICAL CHARACTERIZATION, AND PHARMACOKINETIC STUDY OF DOCETAXEL NANOCRYSTALS

2019 ◽  
pp. 238-244
Author(s):  
ARVIND GANNIMITTA ◽  
PRATHIMA SRINIVAS ◽  
VENKATESHWAR REDDY A ◽  
PEDIREDDI SOBHITA RANI
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Water Solubility ◽  
Release Kinetics ◽  
Tween 80 ◽  
Fickian Diffusion ◽  
Sustained Drug Release ◽  
Egg Lecithin

Objective: The main objective of this study was to prepare and evaluate the nanocrystal formulation of docetaxel. Methods: Docetaxel nanocrystals were formulated to improve the water solubility. Docetaxel nanocrystals were prepared by nanoprecipitation method using Tween 80, egg lecithin, and povidone C-12 as stabilizers and poly(lactic-co-glycolic acid) (PLGA) as polymer in acceptable limits. A total of 16 formulations were prepared by changing stabilizer and polymer ratios. The prepared nanocrystals were characterized by particle size, zeta potential, crystalline structure, surface morphology, assay, saturation solubility, and in vitro drug release. Results: Based on particle size, polydispersity index, and zeta potential data, four formulations were optimized. The formulation containing Tween 80 as stabilizer has shown lowest particle size and better drug release than the formulations containing egg lecithin and povidone C-12 as stabilizers. The formulation containing Tween 80 and PLGA has shown still lower sized particles than the Tween 80 alone and exhibited prolonged sustained drug release. The release kinetics of formulations containing Tween 80 and PLGA followed zero-order release kinetics and formulations containing egg lecithin and povidone C-12 followed Higuchi diffusion (non-Fickian). Conclusion: From the study, we concluded that as the type and concentration of stabilizer changed the size and shape of the crystals were also changed and the formulations showed sustained drug release with non-Fickian diffusion.

scholarly journals Fabrication and in vitro characterization of polymeric nanoparticles for Parkinson's therapy: a novel approach

2014 ◽  
Vol 50 (4) ◽  
pp. 869-876 ◽  
Author(s):  
Neha Gulati ◽  
Upendra Nagaich ◽  
Shubhini Saraf
Keyword(s):  
Drug Release ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Mode Of Delivery ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Fickian Diffusion ◽  
Novel Approach

The objective of the research was to formulate and evaluate selegiline hydrochloride loaded chitosan nanoparticles for the Parkinson's therapy in order to improve its therapeutic effect and reducing dosing frequency. Taguchi method of design of experiments (L9 orthogonal array) was used to get optimized formulation. The selegiline hydrochloride loaded chitosan nanoparticles (SHPs) were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP) and tween 80 as surfactant. The SHPs had a mean size of (303.39 ± 2.01) nm, a zeta potential of +32.50mV, and entrapment efficiency of SHPs was 86.200 ± 1.38%. The in vitro drug release of SHPs was evaluated in phosphate buffer saline (pH 5.5) using goat nasal mucosa and found to be 82.529% ± 1.308 up to 28 h. Release kinetics studies showed that the release of drug from nanoparticles was anomalous (non-fickian) diffusion indicating the drug release is controlled by more than one process i.e. superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. SHPs showed good stability results as found during stability studies at different temperatures as mentioned in ICH guidelines. The results revealed that selegiline hydrochloride loaded chitosan nanoparticles are most suitable mode of delivery of drug for promising therapeutic action.

scholarly journals FORMULATION AND IN-VITRO EVALUATION OF THEOPHYLLINE HYDROCHLORIDE EFFERVESCENT FLOATING TABLETS: EFFECT OF POLYMER CONCENTRATION ON TABLET BUOYANCY

2019 ◽  
pp. 59-65
Author(s):  
AKPABIO E. I. ◽  
EFFIONG D. E. ◽  
UWAH T. O. ◽  
SUNDAY N. I.
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Wet Granulation ◽  
Floating Tablets ◽  
Swelling Characteristics

Objective: This study was undertaken to formulate a floating drug delivery system of theophylline hydrochloride using different concentrations of a chosen polymer and then investigate how polymer concentration affects buoyancy and drug release properties of the tablets. Methods: Hydroxypropyl methylcellulose (HPMC) at different concentration levels of 15% (F1), 20% (F2) and 30% (F3) was used to form the three formulation batches of floating tablets. Wet granulation method was used for the granule preparation while Sodium bicarbonate and citric acid were used as the gas generating agent. The physical properties of the granules and the floating tablets were evaluated. Also determined were the physicomechanical properties, buoyancy and swelling characteristics of the tablets. The in vitro drug release study was carried out according to the USP I (basket method) for 8h in 900 ml 0.1N HCl at 50 rpm. Samples withdrawn at the regular predetermined time were analyzed spectrophotometrically at a wavelength of 271 nm and data obtained statistically analyzed by one-way analysis of variance (ANOVA). The differences between means were considered significant at P<0.05. Results: The result showed that polymer (HPMC) concentration significantly (p>0.05) increased swelling index and improved floating lag time, it had no significant effect on the total floating time. Percentage drug release at the end of 8 h was 100%, 98.2% and 96.13% for formulation F1, F2 and F3, respectively. All three formulations followed the Higuchi drug release kinetics model and the mechanism of drug release was the non Fickian diffusion with exponents of 0.46, 0.51 and 0.56 for the respective batch. Conclusion: Batch F3 gave a better-controlled drug release and floating properties in comparison to batch F1 and F2 thus Polymer concentration influenced the onset of floating and controlled the release of Theophylline.

scholarly journals FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF CIPROFLOXACIN BY SOLVENT EVAPORATION METHOD USING DIFFERENT POLYMERS

2021 ◽  
pp. 101-108
Author(s):  
KAUSLYA ARUMUGAM ◽  
PAYAL D. BORAWAKE ◽  
JITENDRA V. SHINDE
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Angle Of Repose ◽  
Solvent Evaporation Method ◽  
Evaporation Method

Objective: The main intention of this research was to formulate and evaluate floating microspheres of ciprofloxacin using different polymers to prolong gastric residence time. Methods: The microspheres were formulated by the solvent evaporation method using different ratios of polymers like carbopol 940, ethylcellulose, and Hydroxy Propyl Methyl Cellulose K4M. Further, the floating microspheres were evaluated for micromeritic properties like bulk density, tapped density, angle of repose, etc., percentage yield, particle size, entrapment efficiency, floating capacity, in vitro drug release study, release kinetics, drug content, swelling index, and Fourier Transform Infrared Spectroscopy (FTIR) (Compatibility studies). Results: The ciprofloxacin microspheres showed the good flowing property. The particle size ranged from 258.1±2.21 µm to 278±2.86 µm and entrapment efficiency ranged from 63.17±0.43% to 89.90±1.32%. The IR spectrum revealed that there was no interaction between the drug and polymer. F7 formulation was found to be the best formulation. Drug release was found to be 90.70±0.89% i.e. in a controlled manner at the end of 10 h. Conclusion: The floating microspheres were prepared successfully and the results clearly stated that prepared ciprofloxacin microspheres may be safe and effective controlled drug delivery over an extended period which can increase bioavailability, patient compliance, and decrease dosing frequency.

scholarly journals Fabrication and Characterization of Anticancer Drug Loaded Double Walled Microspheres

2019 ◽  
Vol 9 (4-A) ◽  
pp. 79-85
Author(s):  
Elangovan Nagarajan ◽  
B Rama ◽  
M Swetha ◽  
G.S Sharma ◽  
L Jyothi Rani ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Guar Gum ◽  
Diffusion Mechanism ◽  
Polymer Concentration ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Breast Cancer Patients

In the present work, double walled microspheres of Tamoxifen (antiestrogenic drug) using Sodium alginate, Hydroxy propyl methyl cellulose (HPMC) K100,Guar gum, Xanthun gum were formulated to deliver Tamoxifen (TMX) through  oral route to treat breast cancer patients. Details regarding the preparation and evaluation of the formulations have been discussed in results. From the study following conclusions could be drawn. The results of this investigation indicate that Ion gelation method can be successfully employed to fabricate TMX microspheres. FT-IR spectra of the physical mixture revealed that the drug is compatible with the polymers and copolymer used. Microspheres containing sodium alginate along with HPMC in 1:1 ratio had a least size range of 610µm. Increase in the polymer concentration led to increase in % Yield, % Drug entrapment efficiency, Particle size. The  invitro drug release decreased with increase in the polymer and copolymer concentration. Among all formulations F7 shows Maximum drug release in 12 th hr  when compared with other formulations. Analysis of drug release mechanism showed that the drug release from the formulations followed the Non fickian diffusion mechanism and follows zero order kinectics. Based on the results of evaluation tests formulation coded F7 was concluded as best formulation. Keywords : Tamoxifen, sodium alginate, HPMC, Microspheres, Diffusion, Copolymers,  Entrapment efficiency.

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