scholarly journals Elaboration of Charged Poly(Lactic-co-Glycolic Acid) Microparticles for Effective Release of Tranexamic Acid

Polymers ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 808
Author(s):  
Ming-Hsi Huang ◽  
Shun-Ying Huang ◽  
Yi-Xuan Chen ◽  
Cheng-You Chen ◽  
Yung-Sheng Lin
Keyword(s):  
Tranexamic Acid ◽  
Glycolic Acid ◽  
Model Compound ◽  
In Vitro Release ◽  
Double Emulsion ◽  
Scanning Calorimetry ◽  
Solvent Evaporation Process ◽  
Vitro Release ◽  
Thermal Stability Of

In this study, tranexamic acid (TA) was used as a model compound to study the charge effect on the physicochemical properties of poly(lactic-co-glycolic acid) (PLGA) microparticles (MPs). Charged PLGA MPs were elaborated by the incorporation of a quaternary ammonium, cetyltrimethylammonium bromide (CTAB), during the double emulsion solvent evaporation process. Three TA-CTAB-carrying modes of PLGA MPs were designed in the CTAB-free (TA-MP), adsorption (TA-CTABAD), or encapsulation (TA-CTABEN) form. The obtained MPs were characterized by morphology and TA-MP affinity. The experiment revealed that the three prepared MPs were spherical and smooth, with pores on their surfaces. TA-CTABAD had a relatively narrow size distribution, compared with that of TA-MP and TA-CTABEN. The particle sizes of TA-MP, TA-CTABEN, TA-CTABAD were measured as 59 ± 17, 54 ± 20, and 19 ± 8 μm, respectively. The zeta potential of the three MPs was found to be in the order: TA-CTABAD > TA-CTABEN > TA-MP. Differential scanning calorimetry (DSC) indicated that the manufacturing process had no influence on the glass transition temperature of the MPs, which was close to 48 °C. Thermogravimetric analysis illustrated that the presence of CTAB slightly changed the thermal stability of PLGA MPs. In vitro release showed that TA-CTABAD exhibited faster TA release than TA-MP and TA-CTABEN in a basic environment (pH of 13), probably because of electrostatic attraction. At pH = 1, the release of TA from TA-CTABEN was faster than those from TA-MP and TA-CTABAD, probably because of electrostatic repulsion. However, the effect of electrostatic interaction was not significant at pH = 7.4.

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.

Flow-through cell-based in vitro release method for triamcinolone acetonide poly (lactic-co-glycolic) acid microspheres

2020 ◽  
Vol 579 ◽  
pp. 119130 ◽  
Author(s):  
Namita P. Tipnis ◽  
Jie Shen ◽  
Derek Jackson ◽  
Daniel Leblanc ◽  
Diane J. Burgess
Keyword(s):  
Triamcinolone Acetonide ◽  
Glycolic Acid ◽  
In Vitro Release ◽  
Flow Through ◽  
Release Method ◽  
Vitro Release

scholarly journals Development and Characterization of Glimepiride Novel Solid Nanodispersion for Improving Its Oral Bioavailability

2020 ◽  
Vol 88 (4) ◽  
pp. 52
Author(s):  
Mona Qushawy ◽  
Ali Nasr ◽  
Shady Swidan ◽  
Yasmin Mortagi
Keyword(s):  
Solid Dispersion ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Water Soluble ◽  
Production Yield ◽  
Scanning Calorimetry ◽  
Differential Scanning Calorimetry Study ◽  
Drug Content ◽  
Vitro Release

Glimepiride is an antidiabetic drug which is one of the third generation sulfonylureas. It belongs to class II, according to the BCS (Biopharmaceutical Classification System), which is characterized by low solubility and high permeability. The aim of this work was to formulate glimepiride as solid dispersion using water-soluble carriers to enhance its aqueous solubility and thus enhance its bioavailability. Nine formulations of glimepiride solid dispersion were prepared by a solvent evaporation technique using three different carriers (mannitol, polyethylene glycol 6000, and β-cyclodextrin) with three different drug carrier ratio (1:1, 1:3, and 1:6). Formulation variables were optimized using 32 full factorial design. The prepared formulations were evaluated for production yield, drug content, micromeritic properties, thermal analysis, in-vitro release, and in-vivo hypoglycemic effect. All prepared formulations showed high production yield ranged from 98.4 ± 2.8 to 99.8 ± 2.2% and high drug content in the range of 97.2 ± 3.2 to 99.6 ± 2.1%. The micromeritic properties revealed that all prepared glimepiride formulations showed good flowability. The differential scanning calorimetry study revealed the presence of the drug in the more soluble amorphous form. In accordance with the results of in vitro release study, it was found that the solubility of glimepiride was increased by increasing the drug carrier ratio, compared with the pure form of the drug. It was found that F9 showed a high and rapid reduction in blood glucose levels in diabetic rats, which indicated the success of a solid dispersion technique in improving the solubility and hence the bioavailability of glimepiride.

scholarly journals An Injectable Nano-Enabled Thermogel to Attain Controlled Delivery of p11 Peptide for the Potential Treatment of Ocular Angiogenic Disorders of the Posterior Segment

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 176
Author(s):  
Lisa Claire du Toit ◽  
Yahya Essop Choonara ◽  
Viness Pillay
Keyword(s):  
Polyethylene Glycol ◽  
Polyacrylamide Gel Electrophoresis ◽  
Sol Gel ◽  
In Vitro Release ◽  
Double Emulsion ◽  
Controlled Delivery ◽  
Retinal Cell ◽  
Scanning Calorimetry ◽  
Effective Prevention

This investigation focused on the design of an injectable nano-enabled thermogel (nano-thermogel) system to attain controlled delivery of p11 anti-angiogenic peptide for proposed effective prevention of neovascularisation and to overcome the drawbacks of the existing treatment approaches for ocular disorders characterised by angiogenesis, which employ multiple intravitreal injections of anti-vascular endothelial growth factor (anti-VEGF) antibodies. Synthesis of a polyethylene glycol-polycaprolactone-polyethylene glycol (PEG-PCL-PEG) triblock co-polymer was undertaken, followed by characterisation employing Fourier-transform infrared (FTIR) spectroscopy, nuclear magnetic resonance (NMR) spectroscopy and differential scanning calorimetry (DSC) to ascertain the chemical stability and integrity of the co-polymer instituted for nano-thermogel formulation. The p11 anti-angiogenic peptide underwent encapsulation within poly(lactic-co-glycolic acid) (PLGA) nanoparticles via a double emulsion solvent evaporation method and was incorporated into the thermogel following characterisation by scanning electron microscopy (SEM), zeta size and zeta-potential analysis. The tube inversion approach and rheological analysis were employed to ascertain the thermo-sensitive sol-gel conversion of the nano-thermogel system. Chromatographic assessment of the in vitro release of the peptide was performed, with stability confirmation via Tris-Tricine PAGE (Polyacrylamide Gel Electrophoresis). In vitro biocompatibility of the nano-thermogel system was investigated employing a retinal cell line (ARP-19). A nanoparticle size range of 100–200 nm and peptide loading efficiency of 67% was achieved. Sol-gel conversion of the nano-thermogel was observed between 32–45 °C. Release of the peptide in vitro was sustained, with maintenance of stability, for 60 days. Biocompatibility assessment highlighted 97–99% cell viability with non-haemolytic ability, which supports the potential applicability of the nano-thermogel system for extended delivery of peptide for ocular disorder treatment.

In Vitro Release and Degradation Study of Letrozole-Loaded Poly(Lactic-co-Glycolic Acid) Microparticles

JOM ◽  
2020 ◽  
Vol 73 (1) ◽  
pp. 450-459
Author(s):  
Akhtar Jahan Siddiqa ◽  
Nilesh Kumar Shrivastava ◽  
M. E. Ali Mohsin ◽  
Mustufa Haider Abidi ◽  
Mohamed Abdel Fattah Sharaf ◽  
...  
Keyword(s):  
Glycolic Acid ◽  
In Vitro Release ◽  
Degradation Study ◽  
Vitro Release

scholarly journals DESIGN, OPTIMIZATION AND IN VITRO EVALUATION OF ANTIFUNGAL ACTIVITY OF NANOSTRUCTURED LIPID CARRIERS OF TOLNAFTATE

2019 ◽  
pp. 109-115
Author(s):  
AHMED GARDOUH ◽  
Samar H. Faheim ◽  
Samar M. Solyman
Keyword(s):  
Zeta Potential ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Homogenization Method ◽  
Nanostructured Lipid Carriers ◽  
Scanning Calorimetry ◽  
Release Study ◽  
Vitro Release

Objective: The main purpose of this work was to prepare tolnaftate (TOL) loaded nanostructured lipid carriers (NLCs), Evaluate its characteristics and in vitro release study. Methods: Tolnaftate loaded Nanostructured lipid carriers were prepared by the high shear homogenization method using different liquid lipids types (DERMAROL DCO® and DERMAROL CCT®) and concentrations, different concentration ratios of tween80® to span20® and different homogenization speeds. All the formulated nanoparticles were subjected to particle size (PS), zeta potential (ZP), polydispersity index (PI), drug entrapment efficiency (EE), Differential Scanning Calorimetry (DSC), Transmission Electron microscopy (TEM), release kinetics and in vitro release study was determined. Results: The results revealed that NLC dispersions had spherical shapes with an average size between 154.966±1.85 nm and 1078.4±103.02 nm. High entrapment efficiency was obtained with negatively charged zeta potential with PDI value ranging from 0.291±0.02 to 0.985±0.02. The release profiles of all formulations were characterized by a sustained release behavior over 24 h and the release rates increased as the amount of surfactant decreased. The release rate of TOL is expressed following the theoretical model by Higuchi. Conclusion: From this study, It can be concluded that NLCs are a good carrier for tolnaftate delivery

scholarly journals Improvement of In vitro release of Glibenclamide using Cyclodextrin inclusion complexation

2015 ◽  
Vol 13 (1) ◽  
pp. 15-21 ◽  
Author(s):  
Neelkant Prasad ◽  
Navneet Garud ◽  
Akanksha Garud
Keyword(s):  
Complex Formation ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Inclusion Complexation ◽  
Aqueous Solubility ◽  
Scanning Calorimetry ◽  
Hypoglycemic Agent ◽  
Cyclodextrin Inclusion ◽  
Vitro Release

The present study aimed to improve the aqueous solubility of the oral hypoglycemic agent, glibenclamide (GLI), so as to improve its oral absorption, and hence bioavailability after oral administration. This was accomplished by complex formation between GLI and ?-cyclodextrin (?-CD). The study involves the preparation of the inclusion complexes using different techniques. Differential Scanning Calorimetry (DSC) and XRay Diffractometry (XRD) results confirmed the complex formation between GLI and ?-CD. The solubility increase of GLI was due to 1:1 complex formation. The dissolution rate of GLI from the complex prepared by neutralization method was more rapid as compared to other methods used. DOI: http://dx.doi.org/10.3329/dujps.v13i1.21855 Dhaka Univ. J. Pharm. Sci. 13(1): 15-21, 2014 (June)

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