scholarly journals DESIGN, FORMULATION AND EVALUATION OF LIPOSOME CONTAINING ISONIAZID

2018 ◽  
Vol 10 (2) ◽  
pp. 52 ◽  
Author(s):  
Akshay Singha Roy ◽  
Sudipta Das ◽  
Arnab Samanta
Keyword(s):  
In Vitro Release ◽  
Particle Diameter ◽  
Weight Ratio ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Release Profile ◽  
Skewed Distribution ◽  
Size Analysis ◽  
Scanning Calorimetry

Objective: The objective of the present study was to formulate and evaluate liposomes loaded with isoniazid.Methods: Liposome of isoniazid was made by thin layer film hydration method. L-α-phosphatidylcholine and cholesterol were used to make multiamellar vesicles. Six batches of liposomes were prepared based on the different weight ratio of L-α-phosphatidylcholine and cholesterol. Differential scanning calorimetry (DSC) study conducted to study in any incompatibility.Results: The prepared liposomes were evaluated by particle size analysis, entrapment efficiency, release study and stability study. Particle sizes were determined from the scanning electron microscopy (SEM) photographs. When particle frequencies were plotted against particle diameter in the histogram, it showed that F1 batch had a skewed distribution towards smaller liposomes while F6 shows a proper bell-shaped curve with a mean at 225 mm. The percentage entrapment efficiency was found to be 8.99 ± 0.15 to 4.19 ± 0.12 % respectively. From the release profile, it was seen that F1 batch was fastest and F6 was slowest to release the drug. The satisfactory batch F1 was packed in Eppendorf tube and stored at 4 °C temperature for one month. At the end of one month, the samples were analyzed for their physical properties, drug entrapment and in vitro release profile. The percentage release was found to be 96.5 ± 3.2 after 4 h.Conclusion: The F1 batch showed most promising results compared to other. No significant change was found during one month’s stability study of final batch (F1).

scholarly journals TRIVALENT ION CROSS-LINKED AND ACETALATED GELLAN GUM MICROSPHERES OF GLIMEPIRIDE

2020 ◽  
pp. 66-68
Author(s):  
SUDIPTA DAS ◽  
RIMI DEY
Keyword(s):  
In Vitro Release ◽  
Microscopic Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Release Profile ◽  
Gellan Gum ◽  
Long Term Stability ◽  
Vitro Release

Objectives: A novel formulation was developed with glimepiride loaded trivalent ion Al+3 cross-linked and acetalated gellan gum microspheres. Methods: The glimepiride loaded microspheres were formulated using sodium alginate and gellan gum. Cross-linking agents used for the microspheres were aluminum chloride (AlCl3) and glutaraldehyde (GA). The evaluation processes of prepared microspheres were carried out by in-vitro release study, swelling index, microscopic analysis, and entrapment efficiency. Results: All the formulations show good entrapment efficiency and the maximum entrapment 84.6% was governed by the formulation (F3) cross-linked by AlCl3 and GA and their obtained mean particle size were 12.46±3.21 μm. Release profile of the formulations revealed the sustained design of the drug, particularly this formulation (F3), releasing approximately 40% over 4 h. Conclusions: From this experiment, it can be accustomed that F3 possesses higher standard formulation than the rest due to good release profile and entrapment efficiency. Therefore, the long term stability study is required for future development of this formulation.

scholarly journals Preparation and Characterization of Nano Structured Lipid Carriers for Ocular Bacterial Infection

2021 ◽  
pp. 8-23
Author(s):  
Shubhangi Aher ◽  
Ravindra Pal Singh ◽  
Manish Kumar
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Tolerance Test ◽  
Stability Study ◽  
Scanning Calorimetry ◽  
Bacterial Conjunctivitis ◽  
Pure Drug

The problem of bacterial conjunctivitis has dramatically increased in recent years due increased pollution and modern lifestyle. The present study was focused to fabricate Sparfloxacin loaded nanostructured lipid carriers (Spar-NLCs) for ophthalmic application to improve ocular penetration of drug and give sustained release of drug to reduce dosing frequency and toxic effect of drug associated with ocular membrane. A regular two-level factorial design was used to optimize the formulation parameters that are significantly affecting the formulation attributes. Spar-NLCs with particle size 171.1 ± 11 nm, zeta potential -49 ± 6.47 mV, entrapment efficiency 89.5 ± 5% and spherical in shape was obtained. Besides this, FTIR spectroscopy, differential scanning calorimetry, and transmission electron microscopy results suggest that the drug is successfully incorporated in NLC and has excellent compatibility with the excipients. In vitro release study follows Korsmeyer peppas model and suggests that 81.35 ± 6.2% release of drug from Spar-NLCs in 12 hours. The result of ex-vivo permeation study demonstrated 349.75 ± 7.3 µg/cm2 of permeation of drug, 44.482 µg cm-2 hr -1 of flux, and 0.1482 cm hr-1 of permeability coefficient which is 1.7 folds higher than pure drug suspension. The antimicrobial activity of Spar-NLCs was better than the pure drug suspension and equivalent to the marketed formulation. Spar-NLC formulation did not showed any ocular damage, swelling, and redness in in -vivo Draize test. The ocular tolerance test (HET-CAM test) also suggests that the Spar-NLC formulation and its excipients were nonirritant to the ocular tissues. The formulation was found to be stable over the three month of stability study. Therefore, this work strongly suggest that Spar-NLCs has higher penetration and extended release of drug which can be effectively used in prevention of bacterial conjunctivitis.

scholarly journals Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo
Keyword(s):  
Controlled Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

Ultra-deformable Liposomes as Flexible Nanovesicular Carrier to Penetrate Versatile Drugs Transdermally

2020 ◽  
Vol 10 (1) ◽  
pp. 12-20
Author(s):  
Gaurav Tiwari ◽  
Ruchi Tiwari ◽  
Rachna Singh ◽  
Awani K. Rai
Keyword(s):  
Skin Permeation ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Human Organ ◽  
Ethanol Injection ◽  
Release Studies ◽  
Junction Protein ◽  
Penetration Ability

Introduction: Transferosomes also known as ultra-deformable liposomes were introduced by Gregor Cevc in 1990. These are deformable vesicles that transport drug across the skin, which is the best route of drug delivery because skin is the largest human organ with 3 kg total weight and a surface area of 1.5-2.0 m2. Methods: Transferosomes are able to efficiently deliver low as well as high molecular weight drug across the skin in terms of quantity and depth. Various methods used for the preparation of transferosomes such as thin film hydration method, reverse phase evaporation method, vortex/sonication method, ethanol injection method and freeze thaw method. Results: The prepared transferosomal preparation will be evaluated for particle shape and size, entrapment efficiency, stability study, penetration ability and skin permeation study. In vitro release studies are to be performed using a specific dissolution medium. Conclusion: Ultra deformable liposomes can be used for delivery of different drugs e.g. analgesic, anesthetic, corticosteroids, anticancer, sex hormone, insulin, gap junction protein, and albumin.

scholarly journals Self-Assembled Casein Nanoparticles Loading Triptolide for the Enhancement of Oral Bioavailability

2020 ◽  
Vol 15 (8) ◽  
pp. 1934578X2094835
Author(s):  
Chengxia Liu ◽  
Ting-ting Jiang ◽  
Zhi-xiang Yuan ◽  
Yu Lu
Keyword(s):  
Self Assembly ◽  
Oral Bioavailability ◽  
In Vitro Release ◽  
Area Under The Curve ◽  
Entrapment Efficiency ◽  
Infrared Spectrometry ◽  
Scanning Calorimetry ◽  
Insoluble Drugs

Triptolide (TP), a broad-spectrum antitumor drug, has very poor solubility and oral bioavailability, which limits its clinical use. Compared with conventional formulations of TP, a casein (Cas)-based drug delivery system has been reported to have significant advantages for the improvement of solubility and bioavailability of insoluble drugs. In this paper, we report the successful preparation of TP-loaded Cas nanoparticles (TP-Cas) using the self-assembly characteristics of Cas in water and the optimization of the formulation by evaluation of entrapment efficiency (EE) and loading efficiency (LE). Dynamic light scattering, transmission electron microscopy, Fourier-transform infrared spectrometry, X-ray diffractometry (XRD), and differential scanning calorimetry (DSC) was adopted to characterize the TP-Cas. Results showed that the obtained TP-Cas were approximately spherical with a particle size of 128.7 ± 11.5 nm, EE of 72.7 ± 4.7 %, and LE of 8.0% ± 0.5%. Furthermore, in vitro release behavior of TP-Cas in PBS (pH = 7.4) was also evaluated, showing a sustained-release profile. Additionally, an in vivo study in rats displayed that the mean plasma concentration of TP after oral administration of TP-Cas was significantly higher than that treated with TP oral suspension. The C max value for TP-Cas (8.0 ± 4.4 μg/mL) was significantly increased compared with the free TP (0.9 ± 0.3 μg/mL). Accordingly, the area under the curve (AUC0-8) of TP-Cas was 2.8 ± 0.8 mg/L·h, 4.3-fold higher than that of TP suspension (0.6 ± 0.1 mg/L·h). Therefore, it can be concluded that TP-Cas enhanced the absorption and improved oral bioavailability of TP. Taking the good oral safety of Cas into consideration, TP-Cas should be a more promising preparation of TP for clinical application.

scholarly journals DIACEREIN-LOADED NIOSOMES (DC-NS): A NEW TECHNIQUE TO SUSTAIN THE RELEASE OF DRUG ACTION

2022 ◽  
pp. 156-163
Author(s):  
RASHAD M. KAOUD ◽  
EMAN J. HEIKAL ◽  
TAHA M. HAMMADY
Keyword(s):  
Physical Stability ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Molar Ratios ◽  
Tween 40 ◽  
A New Technique ◽  
The Stability ◽  
Tween 60

Objective: The study's main goal is to develop a suitable niosomes (NS) encapsulated drug for anti-inflammatory effects such as diacerein (DC) and to evaluate the system's vesicle size (VS), entrapment efficiency (EE %), physical stability and in vitro release. Methods: Tween (40 and 60), cholesterol, and stearylamine were used in a 1:1:0.1 molar ratios as non-ionic surfactants. Thin film hydration was used to create the NS. Results: The higher EE% was observed with NS (F11) prepared from tween 60, cholesterol and 2.5 min sonication. These formulations' release patterns were Higuchi diffusion and first order. For the stability study, NS formulations were stored at temperature between 2-8 °C for 60 d retains the most drugs when compared to room and high temperature conditions. Conclusion: The findings of this study have conclusively shown that after NS encapsulation of DC, drug release is prolonged at a constant and controlled rate.

scholarly journals Development of Epirubicin-Loaded Biocompatible Polymer PLA–PEG–PLA Nanoparticles: Synthesis, Characterization, Stability, and In Vitro Anticancerous Assessment

Polymers ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1212
Author(s):  
Salam Massadeh ◽  
Iman Almohammed ◽  
Eman Barhoush ◽  
Mustafa Omer ◽  
Nouf Aldhawi ◽  
...  
Keyword(s):  
Side Effects ◽  
Double Emulsion ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Synthesis Process ◽  
Free Form ◽  
Scanning Calorimetry ◽  
Biocompatible Polymer ◽  
Mcf 7

Epirubicin (EPI) is an anti-cancerous chemotherapeutic drug that is an effective epimer of doxorubicin with less cardiotoxicity. Although EPI has fewer side effects than its analog, doxorubicin, this study aims to develop EPI nanoparticles as an improved formula of the conventional treatment of EPI in its free form. Methods: In this study, EPI-loaded polymeric nanoparticles (EPI-NPs) were prepared by the double emulsion method using a biocompatible poly (lactide) poly (ethylene glycol) poly(lactide) (PLA–PEG–PLA) polymer. The physicochemical properties of the EPI-NPs were determined by dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), entrapment efficiency and stability studies. The effect of EPI-NPs on cancer cells was determined by high throughput imaging and flow cytometry. Results: The synthesis process resulted in monodisperse EPI-NPs with a size of 166.93 ± 1.40 nm and an elevated encapsulation efficiency (EE) of 88.3%. In addition, TEM images revealed the spherical uniformness of EPI-NPs with no aggregation, while the cellular studies presented the effect of EPI-NPs on MCF-7 cells’ viability; after 96 h of treatment, the MCF-7 cells presented considerable apoptotic activity. The stability study showed that the EPI-NPs remained stable at room temperature at physiological pH for over 30 days. Conclusion: EPI-NPs were successfully encapsulated within a highly stable biocompatible polymer with minimal loss of the drug. The used polymer has low cytotoxicity and EPI-NPs induced apoptosis in estrogen-positive cell line, making them a promising, safe treatment for cancer with less adverse side effects.

scholarly journals Preparation, Characterization, and Acetylcholinesterase Inhibitory Ability of the Inclusion Complex of β-Cyclodextrin–Cedar (Juniperus phoenicea) Essential Oil

Micro ◽  
2021 ◽  
Vol 1 (2) ◽  
pp. 250-266
Author(s):  
Eleni Kavetsou ◽  
Ioanna Pitterou ◽  
Annita Katopodi ◽  
Georgia Petridou ◽  
Abdelaziz Adjali ◽  
...  
Keyword(s):  
Essential Oil ◽  
In Vitro Release ◽  
Release Profile ◽  
Acetylcholinesterase Inhibition ◽  
Precipitation Method ◽  
Scanning Calorimetry ◽  
Juniperus Phoenicea ◽  
Ft Ir ◽  
Co Precipitation

The aim of the present study was the encapsulation of cedar (Juniperus phoenicea) essential oil (CEO) of Greek origin in β-cyclodextrin (β-CD) through the formation of inclusion complexes (ICs) using the co-precipitation method with different β-CD-to-CEO weight ratios (90:10, 85:15, 80:20, 70:30 (w/w)). The encapsulation of CEO in β-CD through host–guest interactions was confirmed by Nuclear Magnetic Resonance (NMR) spectroscopy, FT-IR spectroscopy, Differential Scanning Calorimetry (DSC) and Thermogravimetric Analysis (TGA). The obtained ICs exhibited nanoscale size (315.9 nm to 769.6 nm),Polydispersity Index from 0.326 to 0.604 and satisfactory stability in suspension (−37.0 mV to −17.0 mV). The process yield was satisfactory, ranging between 65% and 78%, while the inclusion efficiency ranged from 10% to 27%. The in vitro release study conducted for the IC with the optimal characteristics (β-CD:CEO 80:20 (w/w)) exhibited a sustained release profile, with an initial burst effect in the first 5 h. The release profile could be well expressed by the Higuchi equation: Q = 18.893 t1/2 + 9.5919, R2 = 0.8491. The cedar EO presented significant acetylcholinesterase inhibition (IC50 37 μg/mL), which was prolonged by its encapsulation into the β-CD cavity.

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 RADITYA ISWANDANA, KURNIA SARI SETIO PUTRI, RANDIKA DWIPUTRA, TRYAS YANUARI, SANTI PURNA SARI, JOSHITA DJAJADISASTRA

2017 ◽  
Vol 9 (5) ◽  
pp. 109
Author(s):  
Raditya Iswandana ◽  
Kurnia Sari Setio Putri ◽  
Randika Dwiputra ◽  
Tryas Yanuari ◽  
Santi Purna Sari ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Tripolyphosphate ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Profile ◽  
Process Efficiency ◽  
Drug Release Profile ◽  
Eudragit L100

Objective: Drug delivery to the colon via oral route can be directly treated a variety of diseases in the colon, such as fibrosis. Tetrandrine is a drug that has anti-fibrosis effects. In this study, chitosan-tripolyphosphate (TPP) beads containing tetrandrine was made and evaluated for in vitro release profile and in vivo targeted test.Methods: Chitosan-TPP tetrandrine beads were prepared by ionic gelation method with variation in sodium tripolyphosphate concentration: 3% (Formula 1), 4% (Formula 2), and 5% (Formula 3). All formulae were characterized for its morphology, particle size, moisture content, process efficiency, entrapment efficiency, thermal character, crystallinity, and swelling. Then, the best formula was coated with HPMCP HP-55, CAP, Eudragit L100-55, or Eudragit L100 prior to drug release profile in vitro and in vivo test.Results: Beads from all formulae had an average size: 920.50±0.04 µm, 942.21±0.08 µm, and 1085.95±0.03 µm; Water content: 7.28±0.003%, 5.64±0.005%, and 6.84±0.004%; Process efficiency: 29.70%, 28.96%, and 29.70%; Entrapment efficiency: 16.20±0.63%, 17.02±0.37%, and 20.42±0.70% for Formula 1, 2, and 3, respectively. In addition, the results of in vitro cumulative drug release were 67.36%, 76.04%, 83.12%, 83.21%, 40.16%, 37.98%, 45.86%, 41.71% for Formula 3A-3H, respectively.Conclusion: It can be concluded that Formula 3D (CAP 15%) was chosen as a formulation with the best in vitro profile. Moreover, the in vivo targeted test showed that Formula 3D was able to deliver the beads to the intestine compared to the control beads.

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