scholarly journals Antitumor efficacy of Folic Acid conjugated Polymeric Nanoparticles of SN-38 after oral delivery

2019 ◽  
Vol 9 (4-s) ◽  
pp. 322-331
Author(s):  
Prasad Shilpi ◽  
J.S Dangi
Keyword(s):  
Particle Size ◽  
Folic Acid ◽  
Oral Delivery ◽  
Tumor Regression ◽  
Polymeric Nanoparticles ◽  
In Vitro Release ◽  
Colon Tumor ◽  
Irinotecan Hydrochloride ◽  
Vitro Release

The objective of the present research was to develop folic acid conjugated polymeric nanoparticles (FCsPNP) and to investigate its therapeutic effectiveness in xenograft Colon tumor models after oral delivery. Chitosan coated PLGA nanoparticles (CsPNP) were prepared by polyelectrolyte complexation method and it was further conjugated with Folic acid. Optimized formulation was investigated for particle size, zeta potential, polydispersity index (PdI), % entrapment drug loading and in vitro release. The morphology was observed by SEM and TEM images. Tumor regression studies were conducted on Balb/c mice implanted with Colo-26 cells. FCsPNP were successfully prepared and optimized. In vitro parameters viz. Particle size, Zeta potential, PdI were found to be optimum. The in vitro % release is directly correlated with the nature of polymers and folate conjugation. In vivo tumor regression studies found the formulations to be less toxic than Irinotecan hydrochloride (IHCl). CsPNP and FCsPNP were successfully prepared and evaluated for antitumor efficacy after oral delivery. FCsPNP were more effective in the colon tumor treatment and found to be less toxic than IHCl thus making it a potential drug delivery candidate for future anticancer therapy. Keywords: Nanoparticles, Xenograft colon tumor, Chitosan, Irinotecan hydrochloride

Development and in vitro and in vivo evaluations of a microemulsion formulation for the oral delivery of oxaprozin

2021 ◽  
Vol 18 ◽  
Author(s):  
Fangming Yin ◽  
Shu Meng ◽  
Xin Zhao ◽  
Huining Wang ◽  
Yingkai Ning ◽  
...  
Keyword(s):  
Particle Size ◽  
Oral Delivery ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Tween 20 ◽  
Peak Time ◽  
Microemulsion Formulation ◽  
Vitro Release

Background: Oxaprozin is labeled as a Class II drug in the biopharmaceutical classification system, and its poor solubility in the entire gastrointestinal tract may be the main reason for its poor oral absorption capacity. Objective: The purpose of this study was to develop an oxaprozin formulation to enhance its oral absorption. Method: Oxaprozin-loaded microemulsions were prepared using the titration method and pseudoternary phase diagram. Characterization experiments were performed on microemulsion preparations, including pH, particle size, shape, zeta potential and stability (thermodynamic, dilution, and differential scanning calorimetry). Then, the in vitro release of the microemulsion and in vivo pharmacokinetics in rats were evaluated. Results : Several microemulsion formulations were prepared. The optimal formulation was 15% oleoyl macrogolglycerides, 35% Tween 20/isopropanol (Km=2) and 50% distilled water. Its particle size met the requirements, and it had a spherical shape with a negatively charged surface. This microemulsion-loaded drug was applied to in vitro release and in vivo pharmacokinetic experiments at 7.47 mg/mL. In vitro release of the oxaprozin-loaded microemulsion best fit the first-order model, while the microemulsion preparation had a certain sustained release effect. In vivo pharmacokinetic experiments indicated that the microemulsion formulation significantly delayed the peak time of the blood concentration and simultaneously prolonged the half-life of drug elimination. Conclusions : The obtained data revealed satisfactory results for this novel microemulsion of oxaprozin, which is very meaningful for clinical trials.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

2017 ◽  
Vol 10 (1) ◽  
pp. 3582-3593
Author(s):  
Chukwuebuka Umeyor ◽  
Uchechukwu Nnadozie ◽  
Anthony Attama
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Carrier System ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Release Study ◽  
Lipid Microparticles ◽  
Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

Preparation, Characterization and In-vitro release of Piroxicam-loaded Solid Lipid Nanoparticles

2010 ◽  
Vol 3 (3) ◽  
pp. 1136-1146
Author(s):  
V K Verma ◽  
Ram A
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Diffusion Method ◽  
Solid Lipid ◽  
Vitro Release

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 

Optimization and Characterization of Aqueous Micellar Formulations for Ocular Delivery of an Antifungal Drug, Posaconazole

2020 ◽  
Vol 26 (14) ◽  
pp. 1543-1555 ◽  
Author(s):  
Meltem E. Durgun ◽  
Emine Kahraman ◽  
Sevgi Güngör ◽  
Yıldız Özsoy
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Size Distribution ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
Glycol Succinate ◽  
Vitro Release

Background: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. Objective: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. Method: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. Results: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. Conclusion: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.

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.

scholarly journals pH-Responsive Liposomes of Dioleoyl Phosphatidylethanolamine and Cholesteryl Hemisuccinate for the Enhanced Anticancer Efficacy of Cisplatin

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 129
Author(s):  
Hassan Shah ◽  
Asadullah Madni ◽  
Muhammad Muzamil Khan ◽  
Fiaz-ud-Din Ahmad ◽  
Nasrullah Jan ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Release Rate ◽  
In Vitro Release ◽  
Chemotherapeutic Agents ◽  
Ph Responsive ◽  
Scanning Calorimetry ◽  
Cholesteryl Hemisuccinate ◽  
Vitro Release

The current study aimed to develop pH-responsive cisplatin-loaded liposomes (CDDP@PLs) via the thin film hydration method. Formulations with varied ratios of dioleoyl phosphatidylethanolamine (DOPE) to cholesteryl hemisuccinate (CHEMS) were investigated to obtain the optimal particle size, zeta potential, entrapment efficiency, in vitro release profile, and stability. The particle size of the CDDP@PLs was in the range of 153.2 ± 3.08–206.4 ± 2.26 nm, zeta potential was −17.8 ± 1.26 to −24.6 ± 1.72, and PDI displayed an acceptable size distribution. Transmission electron microscopy revealed a spherical shape with ~200 nm size. Fourier transform infrared spectroscopic analysis showed the physicochemical stability of CDDP@PLs, and differential scanning calorimetry analysis showed the loss of the crystalline nature of cisplatin in liposomes. In vitro release study of CDDP@PLs at pH 7.4 depicted the lower release rate of cisplatin (less than 40%), and at a pH of 6.5, an almost 65% release rate was achieved compared to the release rate at pH 5.5 (more than 80%) showing the tumor-specific drug release. The cytotoxicity study showed the improved cytotoxicity of CDDP@PLs compared to cisplatin solution in MDA-MB-231 and SK-OV-3 cell lines, and fluorescence microscopy also showed enhanced cellular internalization. The acute toxicity study showed the safety and biocompatibility of the developed carrier system for the potential delivery of chemotherapeutic agents. These studies suggest that CDDP@PLs could be utilized as an efficient delivery system for the enhancement of therapeutic efficacy and to minimize the side effects of chemotherapy by releasing cisplatin at the tumor site.

LINAGLIPTIN AND GLICLAZIDE DI-LOADED EXTENDED-RELEASE NANOPARTICLES: FORMULATION AND EVALUATION

2021 ◽  
Vol 74 (9) ◽  
pp. 2315-2322
Author(s):  
Firas Aziz Rahi ◽  
Muath Sheet Mohammed Ameen ◽  
Mohammed Shamil Fayyadh
Keyword(s):  
Particle Size ◽  
Xanthan Gum ◽  
Extended Release ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Hplc Method ◽  
Electronic Microscopy ◽  
Vitro Release

The aim: This work aimed to formulate gliclazide and linagliptin extended-release nanoparticles. Materials and methods: A HPLC method was developed and validated to determine gliclazide and linagliptin at the same time without interference. The nanoparticles were prepared by emulsion solvent evaporation using two polymers, namely hydroxypropyl methylcellulose (HPMC) 4000 cps and xanthan gum. Results: Nanoparticles prepared were characterized for drug contents, production yield and entrapment efficiency, zeta potential, particle size, morphology by transmission electronic microscopy (TEM) and in-vitro release rate. The formulae GLH1, GLX1 and GHX1 showed release of linagliptin more than 75% after 8 hrs. While the only formula among the three (GHX1) showed release of gliclazide more than 80% after 8 h. So, the formula GHX1 showed acceptable release of more than 80% of both gliclazide and linagliptin after 8 h. Conclusions: The formula GHX1 which containing (0.5:1 xanthan gum: drugs) was the best nanoparticles formula which released more than 80% of both drugs after 8 h and could achieve good extended release over 24 h.

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 Development of NIPAAm-PEG acrylate polymeric nanoparticles for co-delivery of paclitaxel with ellagic acid for the treatment of breast cancer

2019 ◽  
Vol 39 (3) ◽  
pp. 271-278 ◽  
Author(s):  
Suruchi Suri ◽  
Mohd. Aamir Mirza ◽  
Md. Khalid Anwer ◽  
Abdullah S. Alshetaili ◽  
Saad M. Alshahrani ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Particle Size ◽  
Ellagic Acid ◽  
Oral Delivery ◽  
Polymeric Nanoparticles ◽  
Entrapment Efficiency ◽  
Shell Nanoparticles ◽  
Transmission Electron ◽  
Core Shell Nanoparticles

Abstract The aim of the current study was to develop a dual-loaded core shell nanoparticles encapsulating paclitaxel (PTX) and ellagic acid (EA) by membrane dialysis method. Based on particle size, polydispersity index (PDI), and entrapment efficiency, the dual drug-loaded nanoparticles (F2) was optimized. The optimized nanoparticles (F2) showed a particle size of 140±2 nm and a PDI of 0.23±3. The size and the morphology were confirmed by transmission electron microscopy (TEM) and found agreement with the results of dynamic light scattering. The entrapment efficiencies of total drug (PTX and EA), PTX, and EA in the nanoparticles (F2) were measured as 80%, 62.3%, and 37.7%, respectively. The in vitro release profile showed a controlled release pattern for 48 h. A higher cytotoxicity was observed with nanoparticles (F2) in comparison to free PTX. The results revealed that co-delivery of PTX and EA could be used for its oral delivery for the effective treatment of breast cancer.

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