Formulation and Evaluation of Nanosuspension Delivery System for Simvastatin

2014 ◽  
Vol 7 (2) ◽  
pp. 2459-2475 ◽  
Author(s):  
Rupali Shid L. ◽  
Shashikant N. Dhole ◽  
Nilesh Kulkarni ◽  
Santosh L. Shid L.
Keyword(s):  
Zeta Potential ◽  
Dissolution Rate ◽  
Water Soluble ◽  
In Vivo Study ◽  
Diffusion Method ◽  
Total Drug ◽  
Poloxamer 188 ◽  
Drug Content

Poor water solubility and slow dissolution rate are issues polydispersity index. The obtained results showed that for the majority of upcoming and existing biologically active  particlesize (nm) and rate of dissolution has been improved compounds. Simvastatin is poorly water-soluble drug and  when nanosuspension prepared with the higher its bioavailability is very low from its crystalline form. The  concentration of PVPK-30 with the higher concentration of purpose of the present investigation was to increase the  PVP K-30 and Poloxamer-188 and lower concentration of solubility and dissolution rate of simvastatin by the  SLS. The partical size and zeta potential of optimized preparation of nanosuspension by Emulsification Solvent  formulation was found to be 258.3 nm and 23.43. The rate Diffusion Method at laboratory scale. Prepared nanosus- of dissolution of the optimized nanosuspension was pension was evaluated for its particle size and in vitro  enhanced (90.02% in 60 min), relative to plain simvastatin dissolution study and characterized by zeta potential, (21% in 60 min), mainly due to the formation of nanosized differential scanning calorimetry (DSC) and X-Ray particles. These results indicate the suitability of 23 factorial diffractometry (XRD), motic digital microscopy, entrapment  design for preparation of simvastatin loaded efficiency, total drug content, saturated solubility study and nanosuspension significantly improved in vitro dissolution in vivo study. A 23 factorial design was employed to study  rate, and thus possibly enhance fast onset of therapeutic the effect of independent variables, amount of SLS (X1), drug effect. In vivo study shows increase in bioavailability in amount of PVPK-30 (X2) and Poloxamer-188 (X3) and  nanosuspension formulation than the plain simvastatin dependent variables are total drug content and drug. 

Formulation and Evaluation of Nanosuspension Formulation for Drug Delivery of Simvastatin

2014 ◽  
Vol 7 (4) ◽  
pp. 2650-2665
Author(s):  
Rupali L. Shid ◽  
Shashikant N. Dhole ◽  
Nilesh Kulkarni ◽  
Santosh L. Shid
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
In Vivo Study ◽  
In Vitro Dissolution ◽  
Diffusion Method ◽  
Total Drug ◽  
Poloxamer 188 ◽  
Drug Content

Poor water solubility and slow dissolution rate are issues drug content and polydispersity index. The obtained for the majority of upcoming and existing biologically results showed that particle size (nm) and rate of active compounds. Simvastatin is poorly water-soluble  dissolution has been improved when nanosuspension drug and its bioavailability is very low from its crystalline prepared with the higher concentration of PVPK-30 and form. The purpose of the present investigation was to Poloxamer-188 and lower concentration of SLS. The increase the solubility and dissolution rate of simvastatin by particle size and zeta potential of optimized formulation the preparation of nanosuspension by Emulsification was found to be 258.3 nm and 23.43. The rate of Solvent Diffusion Method at laboratory scale. Prepared dissolution of the optimized nanosuspension was nanosuspension was evaluated for its particle size and enhanced (90.02% in 60min), relative to plain simvastatin in vitro dissolution study and characterized by zeta (21% in 60 min), mainly due to the formation of nanosized potential, differential scanning calorimetry (DSC) and particles. These results indicate the suitability of 23 factorial X-Ray diffractometry (XRD), Motic digital microscopy, design for preparation of simvastatin loaded nanosus- entrapment efficiency, total drug content, saturated pension significantly improved in vitro dissolution rate, solubility study and in vivo study. A 23 factorial design was and thus possibly enhance fast onset of therapeutic drug employed to study the effect of independent variables, effect. In vivo study shows increase in bioavailability in amount of SLS (X1), amount of PVPK-30 (X2) and nanosuspension formulation than the plain simvastatin Poloxamer-188 (X3) and dependent variables are Total drug. 

Formulation and Evaluation of Nanosuspension of Simvastatin

2015 ◽  
Vol 8 (2) ◽  
pp. 2858-2873
Author(s):  
Rupali L. Shid ◽  
Shashikant N. Dhole ◽  
Nilesh Kulkarni ◽  
Santosh L Shid
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Factorial Design ◽  
Dissolution Rate ◽  
In Vitro Dissolution ◽  
Total Drug ◽  
23 Factorial Design ◽  
Rate Of Dissolution

Poor water solubility and slow dissolution rate are issues for the majority of upcoming and existing biologically active compounds. Simvastatin is poorly water-soluble drug and its bioavailability is very low from its crystalline form. The purpose of this study wasto increase the solubility and dissolution rate of simvastatin by the  preparation of nanosuspension by emulsification solvent diffusion method at laboratory scale. Prepared nanosus-pension was evaluated for its particle size and in vitro dissolution study and characterized by zeta potential,differential scanning calorimetry (DSC) and X-Ray diffractometry (XRD), motic digital microscopy, entrapment efficiency, total drug content, saturated solubility study and in vivo study. A 23 factorial design was employed to study the effect of independent variables, amount of SLS (X1), amount of PVPK-30 (X2) and poloxamer-188 (X3) and dependent variables are total drug content and polydispersity Index. The obtained results showed that particle size (nm) and rate of dissolution has been improved when nanosuspension prepared with the higherconcentration of PVPK-30 with the higher concentration of PVP K-30 and Poloxamer-188 and lower concentration of SLS. The particle size and zeta potential of optimized formulation was found to be 258.3 nm and 23.43. The rate of dissolution of the optimized nanosuspension was enhanced (90% in 60min), relative to plain simvastatin  (21% in 60 min), mainly due to the formation of nanosized particles. These results indicate the suitability of 23 factorial  design for preparation of simvastatin loaded nano-suspension significantly improved in vitro dissolution rate and thus possibly enhance fast onset of therapeutic drug effect. In vivo study shows increase in bioavailability in nanosuspension formulation than the plain simvastatin drug.

AN ENHANCEMENT OF SOLUBILITY OF PIOGLITAZONE HYDROCHLORIDE USING LIQUISOLID TECHNIQUE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (06) ◽  
pp. 36-39
Author(s):  
S Deshmane ◽  
◽  
K Gandhi ◽  
S. Nagpure ◽  
A. Sawant ◽  
...  
Keyword(s):  
Mathematical Model ◽  
Drug Release ◽  
Dissolution Rate ◽  
In Vivo Study ◽  
Dimethyl Acetamide ◽  
Volatile Liquid ◽  
Ft Ir ◽  
Ir Study

The new mathematical model was developed by studying angle of slide using N, N-dimethyl acetamide, non-volatile liquid vehicle and prepared liquisolid tablets, in which the different concentrations of non-volatile liquid adsorbed over carrier and coating material separately. Both DSC and FT-IR study showed better compatibility and stability. The optimized formulation showed higher drug release during in-vitro and in-vivo study against conventional and marketed preparation. The present work concludes that N, N-dimethyl acetamide enhanced the solubility of pioglitazone HCl with higher dissolution rate through liquisolid technique.

scholarly journals PREPARATION AND CHARACTERIZATION OF NANOCRYSTALS FOR SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF PALIPERIDONE USING DIFFERENT HYDROPHILIC CARRIERS: IN VITRO-IN VIVO STUDY

2018 ◽  
Vol 11 (4) ◽  
pp. 393
Author(s):  
Moon Rajkumar ◽  
Gattani Surendra
Keyword(s):  
Dissolution Rate ◽  
Antipsychotic Agent ◽  
Aqueous Solubility ◽  
In Vivo Study ◽  
Scanning Calorimetry ◽  
Antisolvent Precipitation ◽  
Enhanced Solubility ◽  
Pure Drug

 Objective: The objective of this study was to increase the solubility and dissolution rate of paliperidone (PAL) by preparing its nanocrystals using different hydrophilic carriers by antisolvent precipitation technique.Methods: The nanoparticles (NP) were characterized for aqueous solubility, drug content, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, particle size, and in vitro-in vivo analysis.Results: The results showed improved solubility and dissolution rate of NPs when compared to pure drug and physical mixture (PM). Solubility data showed a linear graph giving an indication that there is a gradual increase in the solubility profile of the drug with an increase in concentration of the carriers. At highest concentration, the solubility of NPs with Plasdone S630, Povidone K-25, and PVP K-30 found to be increased by 12 folds, 9 folds and 6 folds, respectively, as compared to pure drug. The release profile of NPs with Plasdone S630 in terms of dissolution efficiency at 60 min (DE60), initial dissolution rate (IDR), amount release in 15 min (Q15 min), and time for 75% release (t75%) shows better results when compared to pure drug, PM, and also NPs with povidone 25 and povidone 30. In vivo study reveals that optimized NPs elicited significant induction of cataleptic behavior which is the indication of antipsychotic agent(s) effect.Conclusion: The process antisolvent precipitation under constant stirring may be a promising method to produce stable PAL NPs with markedly enhanced solubility and dissolution rate due to nanonization with the increased surface area, improved wettability, and reduced diffusion pathway.

scholarly journals Formulation and Investigation of Lacidipine as a Nanoemulsions

2020 ◽  
Vol 29 (1) ◽  
pp. 41-54
Author(s):  
Rajaa A. Dahash ◽  
Nawal A. Rajab
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Dissolution Rate ◽  
Thermodynamic Stability ◽  
Water Solubility ◽  
Ph Value ◽  
Pharmaceutical Preparations ◽  
Light Transmittance ◽  
Drug Content

Many pharmaceutical molecules have solubility problems that until yet consist a hurdle that restricts their use in the pharmaceutical preparations. Lacidipine (LCDP) is a calcium-channel blocker with low aqueous solubility and bioavailability.         Lipid dosage forms are attractive delivery systems for such hydrophobic drug molecules. Nanoemulsion (NE)  is one of the popular methods that has been used to solve the solubility problems of many drugs. LCDP was formulated as a NE utilizing triacetin as an oil phase, tween 80 and tween 60 as a surfactant and ethanol as a co-surfactant. Nine formulas were prepared, and different tests performed to ensure the stability of the NEs, such as thermodynamic stability, particle size, Polydispersity index, zeta potential, dye solubility test, dilution test, drug content test and in-vitro drug release. Results of characterization showed that LCDP NE (F-5) with (oil: Smix (3:1):DDW (10:60:30)) ratio was selected as a best formula, since it have excellent thermodynamic stability with a particle size of 13.42, low PDI 0.234 , zeta potential (-14.5mV), efficient electrical    conductivity  0.241ms/cm , good pH value (5.9), good percent of light transmittance (99.10%) , with  acceptable viscosity , higher percent of drug content (99.14%) and complete release of the drug after (30 min.) with significantly higher (P<0.05)   dissolution rate in comparison with pure drug powder.      From the results obtained NE was found to be an efficient method to enhance the solubility and dissolution rate of drugs that have poor water solubility (lipophilic drugs).    

scholarly journals Formulation and In-Vitro Evaluation of Meloxicam Solid Dispersion using Natural Polymers.

2021 ◽  
Vol 30 (1) ◽  
pp. 169-178
Author(s):  
Hiba Radhi ALhassani ◽  
Eman B. H. Al-Khedairy
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Oral Absorption ◽  
Chemical Interaction ◽  
Water Soluble ◽  
Natural Polymers ◽  
Drug Content ◽  
Percentage Yield

Meloxicam (MLX) is non-steroidal anti -inflammatory, poorly water soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. Solid dispersion (SD) is an effective technique for enhancing the solubility and dissolution rate of such drug.     The present study aims to enhance the solubility and the dissolution rate of MLX by SD technique by solvent evaporation method using sodium alginate (SA), hyaluronic acid (HA), collagen and xyloglucan (XG) as gastro-protective hydrophilic natural polymers. Twelve formulas were prepared in different drug: polymer ratios and evaluated for their, percentage yield, drug content,  water solubility,  dissolution, crystal lattice using powder X-ray diffraction (PXRD) and studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-polymer interaction. All the prepared showed improvement of drug solubility except that prepared with HA. The best result was obtained with formula SD1 (MLX: SA 1:1) that showed a high percentage yield (97), high drug content (97.4±0.05) and increase in solubility compared to solubility of pure MLX with improved dissolution rate. the PXRD study revealed the conversion of the drug to amorphous form without chemical interaction according to FTIR results

The effect of nanonization on poorly water soluble glibenclamide using a liquid anti-solvent precipitation technique: aqueous solubility, in vitro and in vivo study

RSC Advances ◽  
2015 ◽  
Vol 5 (99) ◽  
pp. 81728-81738 ◽  
Author(s):  
Rohan D. Deshpande ◽  
Gowda D. V. ◽  
Naga Sravan Kumar Varma Vegesna ◽  
Rudra Vaghela ◽  
Kulkarni P. K.
Keyword(s):  
Process Parameters ◽  
Oral Bioavailability ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
In Vivo Study ◽  
Precipitation Technique ◽  
Poorly Water Soluble

In the present study, efforts were made to optimize the process parameters of LAS technique for developing GLB NPs, in order to enhance the aqueous solubility as well as oral bioavailability.

Design, Optimization and in vitro Characterization of Dasatinib loaded PLGA Nano carrier for Targeted cancer therapy: A Preliminary Evaluation

2021 ◽  
pp. 2095-2100
Author(s):  
Shyam S Kumar ◽  
G. Gopalakrishnan ◽  
N. L. Gowrishankar
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Surface Morphology ◽  
Dissolution Rate ◽  
Water Soluble ◽  
Spherical Particles ◽  
Preliminary Evaluation ◽  
Pluronic F68

Objective: Drug nanoparticles offer a versatile platform for enhancing the dissolution rate and bioavailability of poorly water soluble drugs The present study was aimed to design and develop dasatinib (DAS) loaded Poly lactide co glycolic acid (PLGA) to enhance the dissolution rate and to study the effect of formulation variables for the BCS class II drug dasatinib for the treatment of chronic myeloid leukemia. Methods: The DAS loaded Nps were prepared by using modified double emulsion solvent evaporation method (DESE) using different stabilizers, the formulated Nps were characterized for particle size, zeta potential, Poly Dispersity Index, Surface morphology, Drug entrapment and Invitro drug release. Results: The DAS loaded NP s showed the lowest particles size of 123 nm and zeta potential of – results of Pluronic F68 loaded NP showed the lowest particle size of – and highest zeta potential of --. Surface morphology of NPs with DMAB showed distinct smooth spherical particles with the size range of 50nm. Morphology of Pluronic F68 formulated NPs showed the high degree of aggregation. In vitro drug release showed up to 24hrs in a sustained manner. Conclusion: The result of our study indicates the use of PLGA as a sustained release polymer and using DMAB as a stabilizer for better stable formulation.

pH-stabilization of predegraded PDLLA by an admixture of water-soluble sodiumhydrogenphosphate—results of an in vitro- and in vivo-study

Biomaterials ◽  
2002 ◽  
Vol 23 (17) ◽  
pp. 3567-3574 ◽  
Author(s):  
Wolfgang Heidemann ◽  
Stephanie Jeschkeit-Schubbert ◽  
Kurt Ruffieux ◽  
Jürgen Hartmut Fischer ◽  
Hedda Jung ◽  
...  
Keyword(s):  
Water Soluble ◽  
In Vivo Study

scholarly journals Poloxamer-188 and d-α-Tocopheryl Polyethylene Glycol Succinate (TPGS-1000) Mixed Micelles Integrated Orodispersible Sublingual Films to Improve Oral Bioavailability of Ebastine; In Vitro and In Vivo Characterization

Pharmaceutics ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 54
Author(s):  
Nayyer Islam ◽  
Muhammad Irfan ◽  
Salah-Ud-Din Khan ◽  
Haroon Khalid Syed ◽  
Muhammad Shahid Iqbal ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Zeta Potential ◽  
Mixed Micelles ◽  
Entrapment Efficiency ◽  
Glycol Succinate ◽  
Disintegration Time ◽  
Poloxamer 188 ◽  
Pure Drug

Orodispersible sublingual films (OSFs) composed of hydrophilic polymers were loaded with poloxamer-188 and d-α-tocopheryl polyethylene glycol succinate (TPGS-1000) mixed micelles to improve the oral bioavailability of a poorly soluble drug, ebastine (EBT). Mixed micelles formed by thin-film hydration method were incorporated into orodispersible sublingual film, consisting of HPMC and glycerol, using solvent casting technique. The mixed micelles and films were thoroughly evaluated for physicochemical characterization (size, polydispersity index, zeta potential, entrapment efficiency, thickness, weight, surface pH studies, disintegration time, swelling indices, mechanical properties, FTIR, PXRD, DSC, SEM, AFM, in vitro drug release, in vivo bioavailability, and toxicological studies). The results showed that the average particle size of mixed micelles was 73 nm. The mean zeta potential and PDI of the optimal mixed micelles formulation were −26 mV and 0.16, respectively. Furthermore, the maximum entrapment efficiency 82% was attained. The film’s disintegration time was in the range of 28 to 102 s in aqueous media. The integrity of micelles was not affected upon incorporation in films. Importantly, the micelles-loaded films revealed rapid absorption, high permeability, and increased bioavailability of EBT as compared to the pure drug. The existence of ebastine loaded mixed micelles in the films enhanced the bioavailability about 2.18 folds as compared to pure drug. Further, the results evidently established in-vitro and in-vivo performance of bioavailability enhancement, biocompatibility, and good safety profile of micelles-loaded orodispersible EBT films. Finally, it was concluded that film loaded with poloxamer-188/TPGS-1000 mixed micelles could be an effective carrier system for enhancing the bioavailability of ebastine.

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