An Innovative Approach for Development and Evaluation of Nanosized Lamotrigine Loaded Bionanoparticles Using Biopolymer from Fragaria × ananassa Fruit

2020 ◽  
Vol 13 (4) ◽  
pp. 4990-4999
Author(s):  
Sushant Kumar ◽  
Satheesh Madhav N V ◽  
Anurag Verma ◽  
Kamla Pathak
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Kinetic Study ◽  
In Vitro Release ◽  
Release Kinetic ◽  
Fruit Pulp ◽  
Fragaria Ananassa ◽  
Release Study ◽  
Vitro Release

The purpose of this research was to isolate the smart biopolymer from the fruit pulp of Fragaria × ananassa (garden strawberry). We isolated natural fruit pulp to evaluate the potentiality of biopolymer in delivery of nanosized lamotrigine as an antiepileptic drug. Lamotrigine was nanosized by screening its nano-size particle by UV method. The nanosized lamotrigine was used for preparation of bionanoparticles (LF1-LF8) by sonication method. The isolated biopolymer was characterized for DSC, FTIR, NMR, Mass and Zeta particle size analysis. The obtained results confirm its polymeric nature in different analysis. The prepared bionanoparticles showed the release of lamotrigine in sustained manner over 36 hours. The release kinetic study was done by using the BIT-SOFT 1.12 software and T50% and T80%, r2 were calculated. All the formulation showed more than 99.78% drug release. The In-vitro release study of different formulations showed the % drug release from 90.92% to 99.78%. The different formulations were evaluated for the In-vitro release study and release kinetic was studied. The formulation LF5 was found to be the best formulation having T50% of 17 hours and T80% of 29 hours with r2 value of 0.9925. The best formulation LF5 showed up to 90.925% drug release over 36 hours. According to the release kinetic study, the best-fit model was found to be Koresmayer-Peppas and the mechanism of drug release was found to be anomalous transport. The results obtained from different evaluations like percentage entrapment efficiency, particle size, release study, kinetic studies and stability study revealed that isolated biopolymer has good potentiality to form bionanoparticles and it can be safely used as an alternative to synthetic and semisynthetic polymers for the preparation of lamotrigine loaded stable bionanoparticles

scholarly journals FORMULATION OF POLYMERIC NANOSUSPENSION CONTAINING PRAMIPEXOLE DIHYDROCHLORIDE AND HESPERIDIN FOR IMPROVED TREATMENT OF PARKINSON’S DISEASES

2018 ◽  
Vol 11 ◽  
Author(s):  
Somasundaram I
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Drug Content ◽  
Pramipexole Dihydrochloride ◽  
Vitro Release

Aims and Objectives: The present study is to formulate the nanosuspension containing a hydrophilic drug pramipexole dihydrochloride and hesperidin and to increase the drug entrapment efficiency.Methods: Hesperidin and pramipexole dihydrochloride loaded in chitosan nanosuspension is prepared by ionic gelation method using chitosan and tripolyphosphate. There was no incompatibility observed between the drug and polymer through Fourier transform infrared and differential scanning calorimetric. Various other parameters such as particle size, zeta potential, scanning electron microscope, drug content, drug entrapment efficiency, and in vitro release have been utilized for the characterization of nanoparticles.Results and Discussion: The average size of particle is 188 nm; zeta potential is 46.7 mV; drug content of 0.364±0.25 mg/ml; entrapment efficiency of 72.8% is obtained with HPN3 formulation. The PHC1 shows the highest drug release followed by PHC2 due to low concentration of polymer and PHC4 and PHC5 show less drug release due to high concentration of polymer. The in vitro release of PHC3 is 85.2%, initial the burst release is shown which is approximately 60% in 8 h; then, slow release later on drastic reduction in release rate is shown in 24 h. The in vivo study histopathological report confers the effective protective against rotenone induces Parkinson’s.Conclusion: PHC3 was chosen as the best formulation due to its reduced particle size and controlled release at optimum polymer concentration which may be used to treat Parkinson’s disease effectively..

scholarly journals A NOVEL NANOGEL FORMULATION OF FINASTERIDE FOR TOPICAL TREATMENT OF ANDROGENETIC ALOPECIA: DESIGN, CHARACTERIZATION AND IN VITRO EVALUATION

2021 ◽  
pp. 228-240
Author(s):  
DIVYA SANGANABHATLA ◽  
R. SHYAM SUNDER
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Androgenetic Alopecia ◽  
Stability Studies ◽  
Drug Content ◽  
Release Study

Objective: The present paper describes the development and evaluation of a Novel Finasteride (FSD) nanogel topical delivery for the treatment of Androgenetic Alopecia. Nano-based topical formulation was chosen to enhance the solubility, permeability, biocompatibility of drug and to overcome the problems associated with the oral delivery of finasteride. Methods: Various trails batches were prepared by using probe sonication method. Based on stability studies and particle size, NP4 trail was optimized which exhibited a spherical shape with a mean diameter of 113.80±0.72, the polydispersity of 0.28±0.01, zeta potential of-25.2 mV, drug entrapment efficiency of 92.67±0.47 %, and drug loading of 6.15±0.02 %. Storage stability studies demonstrated that the particle size and entrapment efficiency were not changed during 3 mo both at 4 °C and room temperature. Finasteride (FSD) NLCs were characterized for particle size by scanning electron microscope (SEM), chemical state by X-Ray diffraction (XRD), physical stability by centrifugation and thermodynamic stability by Freeze-thaw method. These prepared nanoparticles were transformed into topical nanogel and further evaluated. Results: Among the different trails, C2 trail of NLC gel has shown excellent gelling capacity, clear appearance, good viscosity characteristics and was selected for further evaluation studies. Batches of topical nanogel were characterized through pH, homogeneity, spreadability, viscosity, drug content and in vitro drug release study. Based on pH (6.5-6.8), drug content (91.25±0.9%), spreadability (6.7 cm/sec), C2 batch was subjected to In vitro skin occlusivity study, in-vitro release study and In vitro heamolysis study. Conclusion: The percent cumulative drug release for Finasteride (FSD) gel was found to be 758.52±1.49 µg at 24 h which is quite higher than plain gel and Finasteride (FSD) gel showed maximum occlusiveness and excellent spreadability and found to be stable. In conclusion, prepared Finasteride (FSD) Nanogel could be used with promising potential for the treatment of Androgenetic Alopecia.

Synthesis and Characterization of Alginate-Based Hydrogel Microbeads for Magnesium Release

2016 ◽  
Author(s):  
Shalil Khanal ◽  
Udhab Adhikari ◽  
Nava P. Rijal ◽  
Devdas Pai ◽  
Jagannathan Sankar ◽  
...  
Keyword(s):  
Particle Size ◽  
Tissue Injury ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Synthesis And Characterization ◽  
Average Particle ◽  
Release Study ◽  
Vitro Release

Magnesium injection is a suitable approach for replenishment of its ions (Mg++) during neural or tissue injury and stroke to avoids risks associated with abnormally low level of Mg++ in blood. In this study, alginate encapsulated magnesium sulfate microbeads were fabricated by the electrospraying technique for Mg++ delivery. Microbeads were evaluated for particle size and surface morphology using inverted optical microscopy and scanning electron microscopy (SEM) respectively. Average particle size of 200–500 μm for hydrated and 50–200 μm for dry beads were observed. An in vitro release study of Mg++ was performed; revealing a cumulative release of ∼50% within first 24 h. This strategy can potentially be useful for the targeted local delivery of magnesium at required concentrations and subsequently enhance the therapeutic efficacy of magnesium in treating tissue injury or stroke.

scholarly journals INTEND, DEPICTION IN VITRO AND IN VIVO APPRAISAL OF GLIPIZIDE FLOATING MICROSPHERES USING ETHYL CELLLULOSE AND HYDROXYL PROPYL METHYL CELLULOSE AS POLYMER BY SUBSTANTIALLY MODIFIED METHOD

2016 ◽  
Vol 9 (5) ◽  
pp. 112
Author(s):  
Rishikesh Gupta ◽  
Sk Prajapati ◽  
Snigdha Pattnaik ◽  
Peeyush Bhardwaj
Keyword(s):  
Particle Size ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Size Analysis ◽  
Release Study ◽  
Tapped Density ◽  
Vitro Release

ABSTRACTObjective: The purpose of this research was to formulate and evaluate floating microsphere of glipizide.Methods: Glipizide microsphere containing ethyl cellulose (EC) and hydroxyl propyl methyl cellulose (HPMC) were prepared by solvent evaporationmethod. Polymer to drug ratio affected characteristics of microspheres. Microspheres were discrete, spherical, and perforated form. The microspheresexhibited good floating property and achieved good gastric retention.Result: In vitro performance was evaluated by the usual pharmacopoeial and other tests such as drug polymer compatibility (Fourier transforminfrared scan), yield (%), micrometric properties such as tapped density (%). Compressibility particle size analysis (by optical microscopy), drugentrapment efficiency, surface topography (scanning electron microscope), and in vitro release study. On the basis of results, increasing the polymerratio increased the particle size (195.6±20.24 to 200.89±16.61), increased tapped density (maximum 0.29.60±0.00037 HGF4, batch), and decreased% compressibility (2.13±0.188). Drug loaded floating microspheres were found to be float more than 12 hrs on simulated gastric fluid (pH-1.2).Maximum drug entrapment was found in batch HGF3 (Drug:HPMC:EC) (1:1:3). Electron microscopy showed its perforated surface with hollowness.After 10 hrs, maximum release was found to be 78.0% (batch-GF1).Conclusion: The release study was performed in simulated gastric fluid with 0.02% tween80. The best release result was obtained at the ratio ofdrug: polymer (1:1).Keywords: Floating microspheres, Glipizide, Gastrorentensive system, In vitro release.

scholarly journals Comparative Study of Herbal Extract of Piper Nigrum, Piper Album and Piper Longum on Various Characteristics of Pyrazinamide and Ethambutol Microspheres

2019 ◽  
Vol 9 (4-A) ◽  
pp. 72-78
Author(s):  
Prashant L Pingale ◽  
R. P. Ravindra
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Herbal Extract ◽  
Piper Nigrum ◽  
Equal Proportion ◽  
In Vitro Drug Release ◽  
Piper Longum ◽  
Release Study ◽  
Vitro Release

Bioenhancers are the ‘bioavailability enhancers’; they do not show any therapeutic effect, but when used in combination enhances the activity of drug molecule. In a cited research paper, the effect of various species of piper used as bioenhancer singly and in combination in an equal ratio. The methods used for preparation of microspheres are Complex Coacervation and Modified Emulsion Method. The prepared microspheres were evaluated for various parameters like in-vitro release, drug entrapment efficiency, percent bioadhesion, permeability study using intestinal sac method. The in-vitro drug release of drugs from formulations where Piper nigrum was used as bioenhancers was found to be about 66-70% in 12 hrs. when used singly. When bioenhancers used in combination the in-vitro drug release of drugs was increased up to 85-90% for combination of Piper album and Piper longum in an equal proportion, the same was about 35-40% in case of formulations where no bioenhancers was used. The microspheres found to be less than 130 micron in size. The DEE was found to be in the range of 27-67%. The bioadhesion of the microsphere were found to be 20-76% (increased in formulations where bioenhancers incorporated). The in- vitro release study by USP paddle apparatus, the important results from in-vitro release study relates to the very significant enhancement in drug release, due to presence of bioenhancers. Keywords: Microspheres, Bioenhancer, Piper nigrum, Piper album, Piper longum, Pyrazinamide, Ethambutol

scholarly journals Development of Oral Sustained Release Rifampicin Loaded Chitosan Nanoparticles by Design of Experiment

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Bhavin K. Patel ◽  
Rajesh H. Parikh ◽  
Pooja S. Aboti
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sustained Release ◽  
Design Of Experiment ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Kinetic

Objective. The main objective of the present investigation was to develop and optimize oral sustained release Chitosan nanoparticles (CNs) of rifampicin by design of experiment (DOE). Methodology. CNs were prepared by modified emulsion ionic gelation technique. Here, inclusion of hydrophobic drug moiety in the hydrophilic matrix of polymer is applied for rifampicin delivery using CN. The 23 full-factorial design was employed by selecting the independent variables such as Chitosan concentration (X1), concentration of tripolyphosphate (X2), and homogenization speed (X3) in order to achieve desired particle size with maximum percent entrapment efficiency and drug loading. The design was validated by checkpoint analysis, and formulation was optimized using the desirability function. Results. Particle size, drug entrapment efficiency, and drug loading for the optimized batch were found to be 221.9 nm, 44.17 ± 1.98% W/W, and 42.96 ± 2.91% W/W, respectively. In vitro release data of optimized formulation showed an initial burst followed by slow sustained drug release. Kinetic drug release from CNs was best fitted to Higuchi model. Conclusion. Design of Experiment is an important tool for obtaining desired characteristics of rifampicin loaded CNs. In vitro study suggests that oral sustained release CNs might be an effective drug delivery system for tuberculosis.

scholarly journals ORAL GENTAMICIN PREPARATION USING SOLIDIFIED LIPID PARTICULATE DELIVERY SYSTEM

2017 ◽  
Vol 9 (9) ◽  
pp. 22
Author(s):  
Musiliu Adedokun ◽  
Tenderwealth Jackson ◽  
Kelechi Uchegbu ◽  
Anthony Attama
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Delivery System ◽  
In Vitro Release ◽  
Zero Order ◽  
Lipid Matrix ◽  
Mean Particle Size ◽  
Release Study ◽  
Vitro Release

Objective: Despite the broad pharmacological activity of gentamicin against a number of bacteria, it's very inadequate oral bioavailability due to poor intestinal membrane permeability has limited its formulation into oral dosage delivery system. This work was thus aimed at formulation and evaluation of gentamicin-loaded microemulsions based on preparation of lipid matrix for sustained release delivery.Methods: Oral gentamicin suspensions were prepared by emulsification method using Tween 80 as a mobile surfactant in the lipid matrix dispersion. The resultant oral suspensions were evaluated for mean particle size and morphology using a photomicrograph, encapsulation efficiency/entrapment, EE (%), dispersibility, pH and absolute drug content. Release study as a function of inhibition zone diameter (IZD) and in vitro release study was also carried out. The in vitro release study was performed in both simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.2) respectively. The release data were analyzed mathematically according to zero order, first order and Higuchi equations.Results: The prepared suspensions were cream-white in colour, easily dispersed and well homogenized. Batch D, which had least amount of excipients incorporated into the lipid matrix showed clumped irregular-shaped and less free-flowing particles. The particle size was significantly influenced by lipid matrix combination ratio in the presence of a surfactant (p<0.05). The mean particle size diameters of the samples were 15.44 mm, 10.64 mm, 4.12 mm, and 2.70 mm for batches A, B, C and D respectively. The values of EE obtained varied between 47% and 59% with Batch B exhibiting the highest value. The Higuchi model gave the best release kinetics result followed by zero order kinetics.Conclusion: Oral gentamicin prepared exhibited antibacterial properties against Klebsiella spp., Escherchia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa. The results suggest that a lipid matrix system could be useful as a sustained release oral delivery system of a poorly absorbable drug such as gentamicin.

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