Development of Controlled-Release Carbamide Peroxide Loaded Nanoemulgel for Tooth Bleaching: In Vitro and Ex Vivo Studies

Burst release of carbamide peroxide (CP) from traditional hydrogels causes severe inflammation to periodontal tissues. The present study explores the development of a novel CP nanoemulgel (CP-NG), an oil-in-water nanoemulsion-based gel in which CP was loaded with a view to controlling CP release. CP solid dispersions were prepared, using white soft paraffin or polyvinylpyrrolidone-white soft paraffin mixture as a carrier, prior to formulating nanoemulsions. It was found that carrier type and the ratio of CP to carrier affected drug crystallinity. Nanoemulsions formulated from the optimized CP solid dispersions were used to prepare CP-NG. It was found that the ratio of drug to carrier in CP solid dispersions affected the particle size and zeta potential of the nanoemulsions as well as drug release behavior and tooth bleaching efficacy of CP-NG. Drug release from CP-NG followed a first-order kinetic reaction and the release mechanism was an anomalous transport. Drug release rate decreased with an increase in solid dispersion carriers. CP-NG obtained from the solid dispersion with a 1:1 ratio of CP to the polymer mixture is suitable for sustaining drug release with high tooth bleaching efficacy and without reduction of enamel microhardness. The developed CP-NG is a promising potential tooth bleaching formulation.

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Enhancing Stability and Tooth Bleaching Activity of Carbamide Peroxide by Electrospun Nanofibrous Film

Pharmaceuticals ◽

10.3390/ph13110381 ◽

2020 ◽

Vol 13 (11) ◽

pp. 381

Author(s):

Siriporn Okonogi ◽

Adchareeya Kaewpinta ◽

Thomas Rades ◽

Anette Müllertz ◽

Mingshi Yang ◽

...

Keyword(s):

Drug Release ◽

Ex Vivo ◽

Pure Water ◽

Entrapment Efficiency ◽

Tooth Bleaching ◽

Release Mechanism ◽

Carbamide Peroxide ◽

Human Teeth ◽

Bleaching Efficiency ◽

Bleaching Activity

Carbamide peroxide (CP) possesses a strong tooth bleaching activity, however, its clinical application is limited because of its instability in aqueous formulations. This study explores the improvement of CP stability and bleaching activity by loading CP in electrospun nanofibrous film (ENF). Polyvinylalcohol, polyvinylpyrrolidone, and silica were used as components for core-based nanofibers of ENF. Electrospinning feed aqueous solutions (EFASs) were developed for preparing CP loaded ENF (CP-ENF). Stability of CP in EFASs is significantly higher than in pure water. The highest stability of CP is found in PPS-CP3, composed of 0.5% CP, 5.5% polyvinylalcohol, 3% polyvinylpyrrolidone, and 1% silica. The results from X-ray diffraction indicate that CP is dispersed as a non-crystalline form in CP-ENFs. CP and the compositions of EFASs play a major role on characteristics and bleaching efficiency of CP-ENFs. Drug release of CP-ENFs is the first order kinetics. CP-ENF obtained from PPS-CP3 shows the highest drug entrapment efficiency, high adhesion, and suitable sustained release. Drug release mechanism is along with anomalous transport according to Korsmeyer–Peppas model. In an ex vivo study using human teeth, it shows the highest bleaching efficiency among the others. Therefore, CP-ENF obtained from PPS-CP3 is a promising ENF for clinical use.

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Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2018.11.6.7 ◽

2018 ◽

Vol 11 (6) ◽

pp. 4337-4348

Author(s):

Bhikshapathi D. V. R. N. ◽

Srinivas I

Keyword(s):

Central Composite Design ◽

Dissolution Rate ◽

Solid Dispersion ◽

Solid Dispersions ◽

Solvent Evaporation ◽

Release Mechanism ◽

Solvent Evaporation Method ◽

Onset Of Action ◽

Evaporation Method ◽

Central Composite

Repaglinide is a pharmaceutical drug used for the treatment of type II diabetes mellitus, it is characterized with poor solubility which limits its absorption and dissolution rate and delays onset of action. In the present study, immediate release solid dispersion of repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of repaglinide.

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Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

Advanced Pharmaceutical Bulletin ◽

10.15171/apb.2019.026 ◽

2019 ◽

Vol 9 (2) ◽

pp. 231-240

Author(s):

Khosro Adibkia ◽

Solmaz Ghajar ◽

Karim Osouli-Bostanabad ◽

Niloufar Balaei ◽

Shahram Emami ◽

...

Keyword(s):

Drug Release ◽

Solid Dispersions ◽

In Vitro Release ◽

Physicochemical Characterization ◽

Amorphous State ◽

Water Soluble ◽

Fickian Diffusion ◽

Release Mechanism ◽

Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

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Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

Journal of Pharmaceutical and Biological Sciences ◽

10.18231/j.jpbs.2021.018 ◽

2021 ◽

Vol 9 (2) ◽

pp. 127-135

Author(s):

Anil Raosaheb Pawar ◽

Pralhad Vitthalrao Mundhe ◽

Vinayak Kashinath Deshmukh ◽

Ramdas Bhanudas Pandhare ◽

Tanaji Dilip Nandgude

Keyword(s):

Ulcerative Colitis ◽

Drug Release ◽

Dissolution Rate ◽

Solid Dispersion ◽

Solid Dispersions ◽

Aqueous Solubility ◽

In Vitro Dissolution ◽

Dissolution Profile ◽

Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

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Facile Construction of Functionalized GO Nanocomposites with Enhanced Antibacterial Activity

Nanomaterials ◽

10.3390/nano9070913 ◽

2019 ◽

Vol 9 (7) ◽

pp. 913 ◽

Cited By ~ 4

Author(s):

Lei Jiang ◽

Zhongjie Zhu ◽

Yanyi Wen ◽

Shan Ye ◽

Chen Su ◽

...

Keyword(s):

Antibacterial Activity ◽

Drug Release ◽

Drug Carrier ◽

Diffusion Method ◽

Release Mechanism ◽

Order Kinetic ◽

Sustained Drug Release ◽

Disk Diffusion Method ◽

Antimicrobial Materials ◽

Inhibition Performance

The development of antimicrobial materials with sustained drug release performance is of great importance. Graphene oxide (GO) is considered to be an ideal drug carrier. In this study, tetracycline hydrochloride (TC) was loaded onto polyethyleneimine-functionalized GO (PG) to fabricate TC/PG nanocomposites. The success of the fabrication was confirmed by zeta potential, TEM, FTIR, and Raman analyses. The TC/PG nanocomposites showed a controlled and sustained drug release behavior, and a pseudo second order kinetic model was employed to illustrate the release mechanism. The antibacterial activity was studied using the disk diffusion method against Escherichia coli and Staphylococcus aureus. The TC/PG nanocomposites exhibited great bacterial inhibition performance. The results indicate that the fabricated TC/PG nanocomposites with effective antibacterial activity have great potential in antibacterial applications.

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Doxorubicin release from optimized electrospun polylactic acid nanofibers

Journal of Industrial Textiles ◽

10.1177/1528083716634033 ◽

2016 ◽

Vol 47 (1) ◽

pp. 71-88 ◽

Cited By ~ 5

Author(s):

Amir Doustgani

Keyword(s):

Differential Scanning Calorimetry ◽

Drug Release ◽

Polylactic Acid ◽

Fiber Diameter ◽

Experimental Result ◽

Coefficient Of Determination ◽

Release Mechanism ◽

Burst Release ◽

Fiber Morphology ◽

Scanning Calorimetry

Electrospinning has been known as an efficient method for fabrication of polymer nanofibers. In this study, an electrospun nanofibrous mats based on polylactic acid with a defined release using doxorubicin was developed. The effects of process parameters, such as concentration, distance, applied voltage, temperature and flow rate on the mean diameter of electrospun doxorubicin-loaded polylactic acid nanofibers were investigated. The fiber morphology and mean fiber diameter of prepared nanofibers were investigated by scanning electron microscopy. Differential scanning calorimetry was employed to identify the presence of doxorubicin within nanofibers. Response surface methodology based on a five-level, five-variable central composite design was used to model the average diameter of electrospun polylactic acid/doxorubicin nanofibers. Mean fiber diameter was correlated to these variables by using a polynomial function at a 95% confidence level. The coefficient of determination of the model was found to be 0.93. The predicted fiber diameter was in good agreement with the experimental result. Differential scanning calorimetry results showed that the doxorubicin was loaded into the nanofibers successfully. In vitro drug release in phosphate-buffered solution and acetate buffer for the optimized and non-optimized samples demonstrated that diffusion is the dominant drug release mechanism for drug-loaded fibers. The initial burst release was observed for non-optimized nanofibers compared to optimized nanofibers. Optimized drug-loaded polylactic acid nanofibers could be good candidates for biomedical applications.

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Solid dispersion of meloxicam: Factorially designed dosage form for geriatric population

Acta Pharmaceutica ◽

10.2478/v10007-007-0048-y ◽

2008 ◽

Vol 58 (1) ◽

pp. 99-110 ◽

Cited By ~ 17

Author(s):

Deepa Pathak ◽

Sunita Dahiya ◽

Kamla Pathak

Keyword(s):

Drug Release ◽

Solid Dispersion ◽

Dosage Form ◽

Solid Dispersions ◽

Methyl Cellulose ◽

Water Soluble ◽

Hydroxyethyl Cellulose ◽

Scanning Calorimetry ◽

Geriatric Population ◽

Peg 4000

Solid dispersion of meloxicam: Factorially designed dosage form for geriatric populationThe objective of the present work was to improve the dissolution properties of the poorly water-soluble drug meloxicam by preparing solid dispersions with hydroxyethyl cellulose (HEC), mannitol and polyethylene glycol (PEG) 4000 and to develop a dosage form for geriatric population. Differential scanning calorimetry, X-ray diffractometry, Fourier transform infrared spectroscopy and scanning electron microscopy were used to investigate the solid-state physical structure of the prepared solid dispersions. Higher invitrodissolution of solid dispersions was recorded compared to their corresponding physical mixtures and the pure drug. PEG 4000 in 1: 9 drug to carrier ratio exhibited the highest drug release (100.2%), followed by mannitol (98.2%) and HEC (89.5%) in the same ratio. Meloxicam-PEG 4000 solid dispersion was formulated into suspension and optimization was carried out by 23factorial design. Formulations containing higher levels of methyl cellulose and higher levels of either sodium citrate or Tween 80 exhibited the highest drug release.

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Development and Optimization of Osmotically Controlled Asymmetric Membrane Capsules for Delivery of Solid Dispersion of Lycopene

The Scientific World JOURNAL ◽

10.1155/2014/438528 ◽

2014 ◽

Vol 2014 ◽

pp. 1-7 ◽

Cited By ~ 5

Author(s):

Nitin Jain ◽

Rashmi Sareen ◽

Neeraj Mahindroo ◽

K. L. Dhar

Keyword(s):

Drug Release ◽

Osmotic Pressure ◽

Correlation Coefficient ◽

Solid Dispersion ◽

Solid Dispersions ◽

Dip Coating ◽

Asymmetric Membrane ◽

Independent Variables ◽

Coating Method ◽

Dip Coating Method

The aim of the present investigation is to develop and statistically optimize the osmotically controlled asymmetric membrane capsules of solid dispersion of lycopene. Solid dispersions of lycopene withβ-cyclodextrin in different ratios were prepared using solvent evaporation method. Solubility studies showed that the solid dispersion with 1 : 5 (lycopene : β-cyclodextrin) exhibited optimum solubility (56.25 mg/mL) for osmotic controlled delivery. Asymmetric membrane capsules (AMCs) were prepared on glass mold pins via dip coating method. Membrane characterization by scanning electron microscopy showed inner porous region and outer dense region. Central composite design response surface methodology was applied for the optimization of AMCs. The independent variables were ethyl cellulose (X1), glycerol (X2), and NaCl (X3) which were varied at different levels to analyze the effect on dependent variables (percentage of cumulative drug release (Y1) and correlation coefficient of drug release (Y2)). The effect of independent variables on the response was significantly influential. The F18was selected as optimized formulation based on percentage of CDR (cumulative drug release) of 85.63% and correlation coefficient of 0.9994. The optimized formulation was subjected to analyze the effect of osmotic pressure and agitational intensity on percentage of CDR. The drug release was independent of agitational intensity but was dependent on osmotic pressure of dissolution medium.

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FORMULATION AND INVITRO EVALUATION OF SOLID DISPERSION TABLETS OF SILYMARIN

International Journal of Advanced Research ◽

10.21474/ijar01/13917 ◽

2021 ◽

Vol 9 (12) ◽

pp. 363-369

Author(s):

Ayesha Naz ◽

◽

Syeda Kulsum ◽

Mehraj Begum ◽

Mohammed Omer ◽

...

Keyword(s):

Quality Control ◽

Drug Release ◽

Solid Dispersion ◽

Solid Dispersions ◽

Angle Of Repose ◽

Control Parameters ◽

Solvent Evaporation Method ◽

Peg 4000 ◽

Quality Control Parameters ◽

Tapped Density

Objective: The research aims to formulate and evaluate Solid Dispersion tablets of Silymarin. Methods: Solid dispersions of Silymarin were prepared with various concentrations of carriers by using solvent evaporation method. The prepared solid dispersions were compressed into tablets by using 8 mm punch rotary tablet punching machine, with the hardness of 3.5kg /cm2.The formulated tablets were evaluated for various quality control parameters. Results: Silymarin was mixed with various proportions of excipients which showed no drug-excipients interactions. The precompression blend of Silymarin solid dispersions were characterized with respect to angle of repose, bulk density, tapped density, Carrs index and Hausners ratio. The precompression blend of all the batches indicated good to fair flowability and compressibility. Conclusion: The tablet passed all the tests. Among all the formulations F4 formulation containing, Drug and PEG 4000 in the ratio of 1:4 showed good result that is 94.95 % in 60 minutes. As the concentration of polymer increased the drug release was increased. While the formulations containing PEG 6000 showed less release. Hence from the dissolution data it was evident that F4 formulation is the better formulation.

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Sustained release formulation of metformin-solid dispersion based on gelucire 50/13- PEG4000: an in vitro study

International Journal of Drug Delivery ◽

10.5138/09750215.2162 ◽

2017 ◽

Vol 9 (3) ◽

pp. 52

Author(s):

Mumini A Momoh ◽

Calister E Ugwu ◽

Tenderwealth Clement Jackson ◽

Ngumezi C Udodiri

Keyword(s):

Drug Release ◽

Solid Dispersion ◽

Encapsulation Efficiency ◽

Solid Dispersions ◽

In Vitro Study ◽

Release Rates ◽

Release Formulation ◽

Sustained Release Formulation ◽

Peg 4000

<p>Metformin is a hydrophilic hypoglycemic agent with permeability and short half-life problems which leads to its low bioavailability. Solid dispersion is one of the unique approaches, to improve bioavailability profiles of drugs. The aim of this study was to prepare and evaluate solid dispersions (SDs) of metformin with polyethylene glycol 4000 (PEG 4000) and Gelucire®50/13 in order to increase its permeability and bioavailability. Solid dispersions of Metformin containing various ratios of PEG 4000: Gelucire®50/13 (1:1, 1:2, 2:1, 1:4, 4:1 as Batch A, Batch B, Batch C, Batch D and Batch E) were prepared using solvent evaporation and fusion techniques. The physical mixtures which served as controls were also prepared. The SDs were evaluated using encapsulation efficiency, percentage yield. The formulations were also characterized with FTIR and DSC. The in vitro drug release studies were also evaluated. The results obtained showed that solid dispersion formulations at pH, 1.2 and 7.4 demonstrated higher release rates than the pure drug. The SDs showed high drug release rates and encapsulation efficiency (% EE) although Batch C containing PEG 4000 and Gelucire 50/13 in the ratio of 2:1 appeared as the batch with most % EE, drug release with broad melting peak. The release rate of metformin increased with increasing amount of PEG 4000. Batch C, SDs containing PEG 4000 and Gelucire 50/13 in the ratio of 2:1 were found to be the most optimized batch with enhanced encapsulation efficiency, most drug release and therefore, improved permeability and bioavailability of metformin.</p>

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