scholarly journals In-vitro Investigation of Polymeric Lipid Hybrid Nanoparticles (Plhns) Of a Chemotherapeutic Drug for the Treatment of Glioblastoma Multiforme

2021 ◽  
Author(s):  
Sankha Bhattacharya
Keyword(s):  
Particle Size ◽  
Polymeric Nanoparticles ◽  
Tween 80 ◽  
Homogenization Method ◽  
Hybrid Nanoparticles ◽  
In Vitro Drug Release ◽  
Anticancer Effects ◽  
Release Studies ◽  
In Vitro Investigation

PHLNs (polymeric lipid hybrid nanoparticles) are core–shell nanoparticle structures made up of polymer cores and lipid shells that have properties similar to both polymeric nanoparticles and liposomes. Methotrexate (MTX) loaded PLHNPs containing tween 80, phosphatidylcholine, poly D, L-lactic-co-glycolic acid (PLGA) & glyceryl tripalmitate prepared using solvent injection & homogenization method for glioblastoma treatment option. The MTX loaded PLHNPs optimized by Box–Behnken design to minimize particle size, higher entrapment efficacy, and maximize MTX concentration in the brain at 4h. The particle size, entrapment efficacy, concentration of drug in brain at 4h, zeta potential and AUC(Brain)/AUC(Plasma) ratio were in the range of 173.51-233.37nm, 70.56-86.34%, 6.38-12.38 μg/mL, 25.78-36.31mV & 1.02-5.32. in-vitro drug release studies, cellular internalization of optimized formulation against U-87 MG shows good anticancer effects.

scholarly journals Development of nitazoxanide-loaded colon-targeted formulation for intestinal parasitic infections: centre composite design-based optimization and characterization

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Charu Bharti ◽  
Upendra Nagaich ◽  
Jaya Pandey ◽  
Suman Jain ◽  
Neha Jain
Keyword(s):  
Particle Size ◽  
Desirability Function ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Percentage Yield ◽  
Vitro Release ◽  
Selection Of

Abstract Background The current investigation is focused on the development and characterization of Eudragit S100 coated nitazoxanide-loaded microbeads as colon-targeted system utilizing central composite design (CCD) and desirability function. The study initiated with the selection of a BCS class II drug nitazoxanide and its preformulation screening with excipients, selection of polymer and identification of concentration for CCD, selection of optimized formulation based on desirability function, and in vitro release studies in simulated gastric and colonic media and stability studies. A two-factor, three-level CCD was employed with two independent variables, i.e. X1 (chitosan % w/v) and X2 (sodium tripolyphosphate % w/v), and three dependent variables, i.e. Y1 (particle size in micrometres), Y2 (percentage yield) and Y3 (percent entrapment efficiency), were chosen. Additionally, surface morphology, mucoadhesion and in vitro drug release studies were also conducted. Result Chitosan concentration showing maximum entrapment and optimum particle size was selected to formulate chitosan beads. The polynomial equation and model graphs obtained from the Design-Expert were utilized to examine the effect of independent variables on responses. The effect of formulation composition was found to be significant (p ˂ 0.05). Based on the desirability function, the optimized formulation was found to have 910.14 μm ± 1.03 particle size, 91.84% ± 0.64 percentage yield and 84.75% ± 0.38 entrapment efficiency with a desirability of 0.961. Furthermore, the formulations were characterized for in vitro drug release in simulated colonic media (2% rat caecal content) and have shown a sustained release of ∼ 92% up to 24 h as compared to in vitro release in simulated gastric fluid. Conclusion The possibility of formulation in enhancing percentage yield and entrapment efficiency of nitazoxanide and the utilization of CCD helps to effectively integrate nitazoxanide microbeads into a potential pharmaceutical dosage form for sustained release.

Preparation, characterization and in vitro drug release studies of novel polymeric nanoparticles

2006 ◽  
Vol 323 (1-2) ◽  
pp. 146-152 ◽  
Author(s):  
Surendra Nimesh ◽  
Romila Manchanda ◽  
Rupesh Kumar ◽  
Amit Saxena ◽  
Preeti Chaudhary ◽  
...  
Keyword(s):  
Drug Release ◽  
Polymeric Nanoparticles ◽  
In Vitro Drug Release ◽  
Release Studies

scholarly journals FORMULATION AND IN VITRO EVALUATION OF CURCUMIN LOADED JACKFRUIT SEED STARCH NANOPARTICLES

2020 ◽  
pp. 32-35
Author(s):  
JUNMONI NATH
Keyword(s):  
Particle Size ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Infrared Studies ◽  
Drug Entrapment Efficiency ◽  
Starch Nanoparticles ◽  
Vitro Release

Objectives: To meet the above aim the following objectives are undertaken: (1) Isolation of starch from jackfruit seeds and formulation of curcumin loaded jackfruit seed starch nanoparticles (2) In vitro evaluations of the drug loaded nanoparticles Methods: Jackfruit seed starch nanoparticles were prepared by Nanoprecipitation technique. In this technique, jackfruit seed starch was mixed with curcumin and acetone solution using a magnetic stirrer at 600 rpm. To the above solution, water were added dropwise and stirred at room temperature until acetone was completely vaporized. Nanoparticles were separated by centrifugation at 4000 rpm after 40 min. Results: Particle size of prepared nanoparticle formulations was found to be 371 to 411.72 nm with PDI of 0.148 to 0.356. The maximum % drug entrapment was found to be 57.34 % with formulation F5. In vitro release studies showed sustained release of drug till 12 h. Conclusion: The prepared nanoparticles were evaluated for its particle size, drug entrapment efficiency, in vitro drug release study, and surface morphology studies by scanning electron microscopy. The results of Fourier transform infrared studies of 1:1 physical mixture of drug and excipients confirmed the absence of incompatibility. Thus, the study concludes that curcumin loaded jackfruit seed starch nanoparticles were developed successfully by nanoprecipitation, which is expected to enhance the oral bioavailability of curcumin.

DOXORUBICIN LOADED POLYCAPROLACTONE-CHITOSAN NANOSPHERES: FORMULATION, CHARACTERISATION AND IN VITRO EVALUATION

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (11) ◽  
pp. 17-23
Author(s):  
K Prakash ◽  
◽  
Y Phalguna ◽  
D. H. Narayana
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Chemical Interaction ◽  
Release Kinetics ◽  
Double Emulsion ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Ftir Studies ◽  
Release Studies

The present study was aimed to develop and evaluate polycaprolactone–chitosan nanospheres of doxorubicin hydrochloride (DXO) in different drug to polymer ratios using double-emulsion solvent evaporation and solvent diffusion methods. FTIR studies showed that there was no chemical interaction between the drug and polymers. Scanning electron microscopy showed the nanospheres having a discrete spherical structure without aggregation. Prepared nanospheres were characterized for particle size, zeta potential, entrapment efficiency and in-vitro drug release kinetics. Nanospheres showed the particle size of 700±105to770±115 nm with an entrapment efficiency of 66.23±0.11% to 93.62±0.17%. The DXO content was found 76±0.12% to 91±0.36% in several batches. In-vitro drug release studies were performed using the dialysis membrane method. All the drug loaded batches were rendered sustained release over a period of 24 h.

scholarly journals Determination of Pickering Nanoemulsion by Eudragit Rl-100 Nanoparticle as Oral Drug Delivery for Poorly Soluble

2021 ◽  
pp. 197-208
Author(s):  
Ashish Y. Pawar ◽  
Khanderao R. Jadhav ◽  
Sagar S. Patil ◽  
Pallavi R. Jadhav
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Aqueous Phase ◽  
Oral Drug Delivery ◽  
Polymeric Nanoparticles ◽  
Oral Drug ◽  
In Vitro Drug Release ◽  
Eudragit Rl

Objective: The purpose of this research study was to develop Ketoprofen-loaded Pickering nanoemulsion with the help of polymeric nanoparticles [NPs]. The pickering nanoemulsion  formulation is developed using Eudragit RL 100, which has the greater ability to stabilize the formulation as well as it better controls the  release of drug upon oral administration. Method: In the present study, Ketoprofen - loaded Pickering nanoemulsion were prepared using an ultrasonic emulsification process. For the preparation of the Nanoemulsion, an aqueous phase of the nanodispersion of nanoparticle is used while Captex -300 and drug premix is used as oil phase. The nanoemulsion is formulated by using a probe sonicator with different ratios of aqueous phase and oil phase. The preformulation study of polymer or drug is done by FTIR and DSC and the drug - polymer compatibility was confirmed by FTIR. The prepared formulation was evaluated for physical appearance, pH, Viscosity, In vitro drug release, Particle size, Zeta Potential, Polydispersivity index, and transmission electron microscopy and stability. The Formulation is optimized for the different concentrations of the aqueous phase and oil phase with concentrations of drug and polymer. Results: All the prepared formulations show particle size in between 100-500nm hence it indicats formation of nanoemulsion. The zeta potential is -46mv which indicates good stability of formulation. The In vitro drug release shows maximum drug release i.e. 96.93% in 10 hrs which shows that the release of drug is prolonged due to formation of Polymer NPs. Conclusion: Thus the drug release was significantly controlled and slowed down when nanoemulsion is formulated by using NPs in comparison with control. These results fulfilled the objective of the study. This study opens new prospects on the formulation of Pickering nanoemulsion. 

scholarly journals Formulation and in vitro Evaluation of Piroxicam Emulgel

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
Y Bindu Vani ◽  
C. Surya Prakash Reddy
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Evaluation Studies ◽  
Tween 80 ◽  
Zero Order ◽  
In Vitro Drug Release ◽  
Zero Order Kinetics ◽  
Release Studies ◽  
Span 80

The present work is concerned with the formulation and evaluation of Piroxicam emulgel employing carbopol 934 and xanthan gum as polymers. The emulgel is prepared by combining the gel and emulsion. The gel in formulations were prepared by dispersing Carbopol 934 and xanthan gum separately in purified water with constant stirring at a moderate speed and then the pH was adjusted to 4 to 5.4 using Tri-ethanol amine (TEA). The oil phase in the emulsion consists of oleic acid and span-80. The aqueous phase in the emulsion was prepared using Tween-80, propylene glycol and distilled water. The prepared emulgel formulations were subjected to evaluation studies like Physical appearance, rheological studies, estimation of drug content and in-vitro drug release. The appearance of prepared emulgel was white. The pH of the emulgel was found to be 5.4. The in vitro drug release studies revealed that formulation F1 showed 85.20% and formulation F2 showed 79.23% of drug release at the end of 8 hrs. The drug release of F1 formulation follows zero order kinetics.

scholarly journals DEVELOPMENT AND IN VITRO EVALUATION OF 5-FLUOROURACIL NANOPARTICLES BY SALTING OUT TECHNIQUE

2020 ◽  
pp. 166-171
Author(s):  
SAILAJA PB ◽  
JEEVANA JYOTHI B
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Average Particle Size ◽  
Average Particle ◽  
Salting Out ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
S 100 ◽  
Percentage Release

Objectives: At the current miserable state of the prevalence of cancers, there is a need for the development of simple technologies to prepare formulations of anticancer drugs with less economy and investment. Hence, the aim of the present work is to prepare nanoparticles of 5-fluorouracil (5-FU) by simple technique, such as salting out method. Methods: Nanoparticles containing 10 mg of 5-FU were prepared by salting out method using Eudragit-100 as polymer. The prepared nanoparticles were evaluated by particle size, zeta potential, in vitro drug release studies, and drug-excipient interaction studies. Results: Nanoparticles prepared by salting out methods showed higher dissolution rate for formulation F3 and F5 revealed high percentage release of 98.6±0.24 in 60 min and 86.5±0.39% in 120 min. Fourier transform infrared (FTIR) spectra revealed no interaction between drug and excipients used for preparation. Conclusion: 5-FU nanoparticles can be produced successfully by salting out method using drug to polymer (Eudragit S-100) ratio of 1:3 to possess ideal drug release characteristics and average particle size of 205.1 nm.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

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

In Vitro Estimation of Photo-Protective Potential of Pomegranate Seed Oil and Development of a Nanoformulation

2019 ◽  
Vol 15 (1) ◽  
pp. 87-102 ◽  
Author(s):  
Surbhi Dhawan ◽  
Sanju Nanda
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Seed Oil ◽  
Topical Delivery ◽  
Inflammatory Activity ◽  
Pomegranate Seed Oil ◽  
Protective Potential ◽  
Release Studies ◽  
Pomegranate Seed

Background: Since ancient times, people have been using natural resources for photoprotection purposes. One such highly recognised natural agent is pomegranate seed oil, considered as wonder oil owing to the presence of several beneficial phytoconstituents. </P><P> Objective: The study aimed to establish the photoprotective potential of pomegranate seed oil through various in vitro and biochemical studies along with the formation of nanoemulsion, an efficient topical delivery system for the oil. </P><P> Method: Photo-protective potential of the oil was estimated by determining in vitro antioxidant and anti-inflammatory activity, total phenolic content, anti elastase, antihyaluronidase and anticollagenase activities of the oil. Ultrasonication method was used to formulate nanoemulsions. The optimisation was done following the central composite design. The characterisation was done by particle size analysis, zeta potential, polydispersity index, pH, viscosity, stability testing and transmission electron microscopy. The optimised nanoemulsion was loaded into a gel base for topical application and further release studies were carried out. </P><P> Results: The IC50 values of anti-elastase, anti-collagenase and anti-hyaluronidase were found to be 309 mg/ml, 4 mg/ml and 95 mg/ml respectively. The results of anti-oxidant and anti-inflammatory activity were also significant, which thereby established the photo-protective potential of the oil. The optimum batch 2 had particle size 83.90 nm, 0.237 PDI and -5.37 mV zeta potential. The morphology was confirmed by TEM. Batch 2 was incorporated into a gel base and release studies showed 74.12 % release within 7 hours. </P><P> Conclusion: Pomegranate seed oil possesses a potential photo-protective ability. Nanoemulsions proved to be a promising carrier for the topical delivery of the oil.

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