scholarly journals PREPARATION AND CHARACTERIZATION OF ORAL NANOSUSPENSION LOADED WITH CURCUMIN

2018 ◽  
Vol 10 (6) ◽  
pp. 90 ◽  
Author(s):  
Sneha Dekate Shreeram Hirlekar ◽  
Srinivas Bhairy ◽  
Srinivas Bhairy ◽  
Rajashree Hirlekar ◽  
Rajashree Hirlekar
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
High Speed ◽  
Drug Loading ◽  
Research Work ◽  
Release Kinetic ◽  
Pharmacokinetic Studies ◽  
Sprague Dawley ◽  
Saturation Solubility

Objective: The principle objective of the present research work was to improve the bioavailability of curcumin (CUR) by decreasing its particle size. Nanosuspension (NS) of CUR was prepared using poloxamer-188 (P188) as a surfactant. The prepared NSs were characterized for particle size, polydispersity index (PDI), zeta potential, drug loading, saturation solubility, and drug release kinetic studies.Methods: Components required for NS preparation, such as solvent, anti-solvent and surfactant were screened. Precipitation high-speed homogenization (HSH) method was used for the preparation of NS using selected components. Evaluation of NS for particle size, PDI, drug loading, saturation solubility and in vitro drug release was done. Pharmacokinetic studies of the NS in sprague dawley (SD) rats were performed.Results: The particle size, PDI and zeta potential of the optimized formulation was 596.5±5 nm, 0.233±0.010 and-23±2 mV respectively. The pH of all the formulations was in the range of 5-6 which is acceptable when related to drug stability. The optimized formulation showed an increase in saturation solubility in water and phosphate buffer pH 6.8 when compared to plain CUR suspension (S). Results of pharmacokinetic studies indicated that Cmax and AUC0-6 were increased 8 and 10 times respectively from plain CUR S to CUR NS.Conclusion: CUR NS was prepared using P188 as the stabilizer. Amongst various stabilizers screened P188 rendered a stable NS with the particle size in nano range. Pharmacokinetic studies revealed the better performance of CUR NS as compared to plain CUR S.

scholarly journals Evaluation and Optimization of Influence of Permeability Property and Concentration of Polymethacrylic Polymers on Microspheres of Metformin HCl

2014 ◽  
Vol 12 (2) ◽  
pp. 131-141 ◽  
Author(s):  
Ikramul Hasan ◽  
Shovan Paul ◽  
Sharmin Akhter ◽  
Navid Jubaer Ayon ◽  
Md Selim Reza
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Drug Loading ◽  
Liquid Paraffin ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Release Kinetic ◽  
Eudragit Rlpo ◽  
Metformin Hcl

Metformin HCl microspheres were prepared with the aim of increasing its bioavailability and decreasing gastrointestinal side effects by means of sustained action. Eudragit RSPO and Eudragit RLPO, polymers of different permeability characteristics were used to prepare different microspheres. Emulsification solvent evaporation technique using acetone as the internal phase and liquid paraffin as the external phase was the method of choice. Six formulations were prepared using two polymers. The effect of drug loading and polymeric property on the surface morphology, entrapment efficiency, particle size and release characteristics of the microspheres were examined. FTIR and DSC studies established compatibility of the drug with the polymers. SEM studies clearly revealed the effect of drug loading and polymeric nature on the surface morphology of the microspheres. Entrapment efficiencies were within 77.09-97.11% and particle size of all the batches were in the acceptable range. Release data were treated with different mathematical kinetic models. The drug release profile showed that Eudragit RSPO and Eudragit RLPO have opposite effect on drug release. On the other hand, increase in drug loading results in increased drug release. Kinetic modeling of in vitro dissolution profiles revealed that the drug release mechanism varies from diffusion controlled to anomalous type. Dhaka Univ. J. Pharm. Sci. 12(2): 131-141, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17611

scholarly journals FORMULATION AND EVALUATION OF ETHAMBUTOL POLYMERIC NANOPARTICLES

2020 ◽  
pp. 207-217
Author(s):  
MONOWAR HUSSAIN ◽  
ANUPAM SARMA ◽  
SHEIKH SOFIUR RAHMAN ◽  
ABDUL MATIN SIDDIQUE ◽  
TANUKU PAVANI EESWARI
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Compatibility Study ◽  
Bacterial Disease ◽  
Dose Frequency

Objective: Tuberculosis (TB) is an infectious bacterial disease caused by Mycobacterium tuberculosis which most commonly affects the lungs. TB has the highest mortality rate than any other infectious disease occurs worldwide. The main objective of the present investigation was to develop polymeric nanoparticles based drug delivery system to sustain the ethambutol (ETB) release by reducing the dose frequency. Methods: The Preformulation studies of drug ETB were done by physical characterization, melting point determination, and UV spectrophotometric analysis. The ETB loaded nanoparticles were prepared by double-emulsion (W/O/W) solvent evaporation/diffusion technique. The prepared polymeric nanoparticles were evaluated for particle size, polydispersity index, zeta potential, drug entrapment efficiency, drug loading, drug-polymer compatibility study, surface morphology, in vitro drug release, and release kinetics. Results: Based on the result obtained from the prepared formulations, F11 showed the best result and was selected as the optimized formulation. Optimized batch (F11) showed better entrapment efficiency (73.3%), good drug loading capacity (13.21%), optimum particle size (136.1 nm), and zeta potential (25.2 mV) with % cumulative drug release of 79.08% at the end of 24 h. Conclusion: These results attributed that developed polymeric nanoparticles could be effective in sustaining the ETB release over 24 h. Moreover, the developed nanoparticles could be an alternate method for ETB delivery with a prolonged drug release profile and a better therapeutic effect can be achieved for the treatment of tuberculosis.

scholarly journals Formulation and evaluaiton of oxiconazole nitrate loaded nanosponges

2021 ◽  
Vol 11 (3) ◽  
pp. 028-040
Author(s):  
Brunda S ◽  
Suresh V Kulkarni ◽  
Manjunath K ◽  
Pushpalatha D
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Kinetic Studies ◽  
Entrapment Efficiency ◽  
Preliminary Test ◽  
Pharmacological Action ◽  
Diffusion Method ◽  
Release Mechanism ◽  
Release Kinetic

Nanotechnology mediated drug delivery has been reported to enhance the drug efficacy, bioavailability, reduced toxicity and improve patient compliance by targeting the cells and tissues to elicit the desired pharmacological action. The main aim of the study was to formulate and evaluate Oxiconazole nitrate loaded nanosponges. The oxiconazole nitrate nanosponges were prepared by the emulsion solvent diffusion method by using the different polymers (Ethyl cellulose, β-CD, HP-β-CD). The FTIR test is conducted as the preliminary test, by this test there was no interaction between the drug and polymers. Then nanosponges (NS) were evaluated for particle size, poly dispersive index (PDI), zeta potential, entrapment efficiency and invitro drug release. The particle size ranged from 480.60 to 753.46nm, PDI ranged from 0.284 to 0.502, zeta potential from -20.9 to -35.9 mV and entrapment efficiency was ranged from 52.72 to 92.72%. The cumulative percentage release from all nanosponges varied from 73.16 to 97.84 % after 12hours depending upon the drug and polymer ratio and F4 formulation showed highest drug release i.e., 97.84%. The release kinetic studies showed that the release zero order diffusion controlled and the n value (0.713) from the Korsmeyer-Peppa’s model indicated the release mechanism was non-fickian type.

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 Development of a novel intraarticular injection of diclofenac for the treatment of arthritis: a preclinical study in the rabbit model

2021 ◽  
Author(s):  
Xinyuan Wen ◽  
Xiaoqing Huang ◽  
Huosheng Wu
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Rabbit Model ◽  
Intraarticular Injection ◽  
Average Particle ◽  
Prepared Nanoparticles

Purpose: To develop a novel intraarticular injection of diclofenac for the treatment of arthritis. Method: Diclofenac loaded nanoparticles were prepared by a nanoprecipitation technique using Eudragit L 100 as the polymer and polyvinyl alcohol as the surfactant. The nanoparticles were evaluated for particle size, zeta potential, scanning electron microscopy, drug release, encapsulation efficiency, and loading efficiency studies. The optimized nanoparticulate formulation was developed for intra articular injection. Intraarticulate injection was evaluated for pH, appearance, viscosity, osmolarity and syringability studies. The optimized injection formulation was tested in an arthritic model consisting of 25 rabbits. Result: Nanoprecipitation method was found to be suitable for diclofenac nanoparticles. The shape of the prepared nanoparticles was found to be spherical and devoid of any cracks and crevices. The average particle size of a diclofenac nanoparticle was found to range from 87±0.47 to 103±0.26 nm. The zeta potential of the prepared nanoparticles was found to be in the range of 0.598±0.34 to 0.826±0.25 mV. The encapsulation efficiency was found to be between 73.45% to 99.03%, while the drug loading was observed between 10.34 to 35.32%. The percentage drug release at 12 hours was found to range from 73.45% to 99.03%. Conclusion: The developed intraarticular injection was found to be within the physically and chemically accepted limits. Animals treated with the intra articular injection of diclofenac showed a significant reduction in swelling as compares to the other groups.

scholarly journals Formulation and evaluation of lovastatin loaded nanosponges

2021 ◽  
Vol 11 (3) ◽  
pp. 041-056
Author(s):  
Pushpalatha D ◽  
Abdul Waris Khan ◽  
Manjunath K ◽  
Brunda S
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Kinetic Studies ◽  
Entrapment Efficiency ◽  
Preliminary Test ◽  
Pharmacological Action ◽  
Diffusion Method ◽  
Release Mechanism ◽  
Release Kinetic

Nanotechnology mediated drug delivery has been reported to enhance the drug efficacy, bioavailability, reduced toxicity and improve patient compliance by targeting the cells and tissues to elicit the desired pharmacological action. The main aim of the study was to formulate lovastatin loaded nanosponges and to evaluate them. Lovastatin loaded nanosponges were prepared by Emulsion solvent diffusion method using different polymers (Ethyl cellulose, Polyvinyl alcohol, β-cyclodextrin, Pluronic F68, Hydroxy Propyl β- cyclodextrin). The FTIR test is conducted as the preliminary test, by this test there was no interaction between the drug and polymers. Then nanosponges were evaluated for particle size, PDI, zeta potential, SEM, entrapment efficiency and invitro drug release. The particle size ranged from 295.5 to 578.8 nm, PDI ranged from 0.189 to 0.465, zeta potential from -17.3 to -35.96 mV and entrapment efficiency was ranged from 78.38 to 95.77 %. The cumulative percentage release from all nanosponges varied from 66.86 to 96.60% after 12 hours depending upon the drug and polymers ratio andF6 formulation showed highest drug release i.e., 96.60%. The release kinetic studies showed that the release first order diffusion controlled and the n value (0.6017) from the Korsmeyer-Peppa’s model indicated the release mechanism was non-fickian type.

scholarly journals An impact of nanocrystals on dissolution rate of Lercanidipine: Supersaturation and crystallization by addition of solvent to antisolvent

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Dolly Tulsibhai Gadhiya ◽  
Jayvadan K. Patel ◽  
Arti Arjanbhai Bagada
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Dissolution Rate ◽  
High Speed ◽  
Particle Morphology ◽  
In Vitro Dissolution ◽  
Antisolvent Precipitation ◽  
Pvp K30

Abstract Background Nanocrystals of any drug are pure solid drug particles with a mean diameter in nanometer range. Dissolution is a crucial factor for absorption of medicine in case of water-insoluble or poorly soluble drugs. The aim of this study was to develop nanocrystals of a hydrophobic drug, Lercanidipine, by addition of solvent to an antisolvent with high-speed homogenization to achieve dissolution and solubility enhancement. Addition of organic solvent to antisolvent results in genesis of nanosized particles due to fast nucleation process and rapid mixing. The nanosuspension was formulated using PVP K30 as a stabilizer. Further, nanosuspensions were lyophilized to convert into solid nanocrystals using mannitol as a cryoprotectant. The developed nanosuspensions were characterized for particle size, zeta potential, saturation solubility, and in vitro dissolution studies. Lyophilized solid nanocrystals were characterized for FTIR, SEM, XRD, and zeta potential (ζ). Results Central composite design was executed to study influence of amount of stabilizer and solvent to antisolvent ratio (independent variables) on particle size and % drug release at 10 min (dependent variables). The particle size of the developed Lercanidipine nanosuspensions were observed in the range of 302.00 ± 10.58 to 484.33 ± 6.51 nm measured by Zetatrac. A considerable increase was found in the solubility and dissolution rate of the nanocrystals as compared to pure drug. The drug release from Lercanidipine nanosuspensions was increased up to 88.95% within 10 min as compared to pure Lercanidipine which was only 21.53%. The X-ray diffraction study of lyophilized nanocrystals showed sharp and distinct peaks due to an increse in crystallinity of Lercanidipine Particle morphology was studied by scanning electron microscopy revealed that nanoprecipitated particles with lyophilization in the presence of mannitol exhibited dendrite needle-like crystals. Conclusion The nanocrystal development by antisolvent precipitation procedure using methanol as solvent, water as antisolvent, and low amounts of PVP K30 as stabilizer is a very promising and effective method to increase the dissolution rate of Lercanidipine. Graphical abstract

Novel Formulation Development and Evaluation of Nanoparticles Based in Situ Gelling System for The Ophthalmic Delivery of Ciprofloxacin Hydrochloride

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Loading ◽  
In Vitro Release ◽  
Formulation Development ◽  
Ciprofloxacin Hydrochloride ◽  
Potential Value ◽  
The Mean ◽  
In Situ Gelling

Ciprofloxacin hydrochloride loaded Eudragit RS100 nanoparticles were prepared by using w/o/w emulsification (multiple emulsification) solvent evaporation followed by drying of nanoparticles at 50°C. The nanoparticles were further incorporated into the pH-triggered in situ gel forming system which was prepared using Carbopol 940 in combination with HPMC as viscosifying agent. The developed nanoparticles was evaluated for particle size, zeta potential value and loading efficiency; nanoparticle incorporated in situ gelling system was evaluated for pH, clarity, gelling strength, rheological studies, in-vitro release studies and ex-vivo precorneal permeation studies. The nanopaticle showed the mean particle size varying between 263.5nm - 325.9 nm with the mean zeta potential value of -5.91 mV to -8.13 mV and drug loading capacity varied individually between 72.50% to 98.70% w/w. The formulation was clear with no suspended particles, showed good gelling properties. The gelling was quick and remained for longer time period. The developed formulation was therapeutically efficacious, stable and non-irritant. It provided the sustained release of drug over a period of 8-10 hours.

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Formulating SLN and NLC as Innovative Drug Delivery Systems for Non-Invasive Routes of Drug Administration

2020 ◽  
Vol 27 (22) ◽  
pp. 3623-3656 ◽  
Author(s):  
Bruno Fonseca-Santos ◽  
Patrícia Bento Silva ◽  
Roberta Balansin Rigon ◽  
Mariana Rillo Sato ◽  
Marlus Chorilli
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
Average Particle Size ◽  
Delivery Systems ◽  
Average Particle ◽  
Minor Importance ◽  
Routes Of Administration ◽  
Non Invasive

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.

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