Performance and drug release studies of poly (ɛ-caprolactone)/γ-poly (glutamic acid) fibrous membranes

2018 ◽  
Vol 89 (9) ◽  
pp. 1642-1657 ◽  
Author(s):  
Henan Zhan ◽  
Shan Liu ◽  
Xiyu Hu ◽  
Dong Jiang
Keyword(s):  
Drug Release ◽  
Water Solubility ◽  
Fiber Strength ◽  
Composite Membranes ◽  
Controlled Drug Release ◽  
Electrospinning Process ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Fibrous Membranes

Fibrous membranes of poly(ɛ-caprolactone)/γ-poly(glutamicacid) (PCL/γ-PGA) composites were successfully produced via an electrospinning process. In doing so, the water solubility of florfenicol (FF) could be enhanced and the drug release properties of FF could be controlled. The mechanical, morphologic, and thermal properties of the fibrous membranes of PCL/γ-PGA were studied by using an electronic single fiber strength machine, scanning electron microscopy, and differential scanning calorimetry. The wettability of the fibrous membranes of PCL/γ-PGA was also measured as discussed in the subsequent section. Fourier transform infrared spectroscopy was applied in the structural analysis of the PCL/γ-PGA-FF fibrous membranes. The results indicated that FF was well blended in the composite membranes of PCL/γ-PGA. In vitro dissolution tests showed that PCL/γ-PGA (85/15; 8%) as both a biodegradable and biocompatible blend may improve the solubility of FF. Therefore, fibrous membranes of PCL/γ-PGA may represent ideal materials for the controlled drug release in various clinical applications.

Formulation and Evaluation of Benidipine Nanosuspension

2021 ◽  
pp. 4111-4116
Author(s):  
Sejal Patel ◽  
Anita P. Patel
Keyword(s):  
Particle Size ◽  
Water Solubility ◽  
Polymer Concentration ◽  
Oral Route ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
23 Factorial Design ◽  
Selection Of

In the interest of administration of dosage form oral route is most desirable and preferred method. After oral administration to get maximum therapeutic effect, major challenge is their water solubility. Water insoluble drug indicate insufficient bioavailability as well dissolution resulting in fluctuating plasma level. Benidipine (BND) is poorly water soluble antihypertensive drug has lower bioavailability. To improve bioavailability of Benidipine HCL, BND nanosuspension was formulated using media milling technique. HPMC E5 was used to stabilize nanosuspension. The effect of different important process parameters e.g. selection of polymer concentration X1(1.25 mg), stirring time X2 (800 rpm), selection of zirconium beads size X3 (0.4mm) were investigated by 23 factorial design to accomplish desired particle size and saturation solubility. The optimized batch had 408 nm particle size Y1, and showed in-vitro dissolution Y2 95±0.26 % in 30 mins and Zeta potential was -19.6. Differential scanning calorimetry (DSC) and FT-IR analysis was done to confirm there was no interaction between drug and polymer.

scholarly journals Formulation and Pharmacokinetic Evaluation of Ritonavir Floating Tablets in the Management of AIDS

2018 ◽  
Vol 10 (6) ◽  
Author(s):  
R. Shireesh Kiran ◽  
B. Chandra Shekar ◽  
B. Nagendra Babu
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Controlled Drug Release ◽  
In Vitro Dissolution ◽  
Gastric Residence Time ◽  
Dissolution Studies ◽  
Floating Tablet ◽  
Gastro Retentive

In the current study, gastro-retentive tablets of Ritonavir was developed to increase its oral bioavailability using hydrophilic polymers HPMC K 4M, K 15M, and K 100M as release retarding agents. Polyox WSR 303 was chosen as resin, sodium bicarbonate was used as effervescent agents. The tablets were prepared by direct compression method and FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K 100M, Crospovidone, Polyox WSR 303 and sodium bicarbonate, as gas generating agent was choosen as optimized formulation based on the evaluation parameters, floating lag time (33 sec) and total floating time (>24 h) and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product was shown 98.67% and 95.09 ± 5.01% of drug release respectively. From in vivo bioavailability studies, after oral administration of floating tablet containing 100 mg Ritonavir, the Cmax, Tmax, and AUC0–∞ of optimized gastroretentive formulation were found to be 30.11 ± 1.16μg/mL, 8.00±1.23 h and 173 ± 26.34μg*h/ml, respectively. Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for improved bioavailability.

Formulation and Characterization of Nateglinide Nanosuspension by Precipitation Method

2014 ◽  
Vol 7 (4) ◽  
pp. 2685-2691
Author(s):  
Amruta Papdiwal ◽  
Kishor Sagar ◽  
Vishal Pande
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Water Solubility ◽  
Average Particle Size ◽  
Biologically Active ◽  
In Vitro Dissolution ◽  
Precipitation Method ◽  
Average Particle ◽  
Scanning Calorimetry

Poor water solubility and slow dissolution rate are major issues for the majority of upcoming and existing biologically active pharmaceutical compounds. Nateglinide is Biopharmaceutical Classification System Class-II drug that has low solubility and high permeability. The purpose of the present study was to improve the solubility and dissolution rate of Nateglinide by the preparation of nanosuspension by the nanoprecipitation technique. Nateglinide nanosuspension was evaluated for its particle size, in vitro dissolution study, and characterized by differential scanning calorimetry and scanning electron microscopy. The optimized formulation showed an average particle size of 207 nm and zeta potential of -25.8 mV. The rate of dissolution of the optimized nanosuspension was enhanced by 83% in 50 min relative to micronized suspension of nateglinide (37% in 50 min). This improvement was mainly due to the formulation of nanosized particles of Nateglinide. Stability study revealed that nanosuspension was more stable at room temperature and refrigerator condition with no significant change in particle size distribution. These results indicate that the nateglinide loaded nanosuspension may significantly improve in vitro dissolution rate and thereby possibly enhance the onset of therapeutic effect.

scholarly journals Combined Self-Nanoemulsifying and Solid Dispersion Systems Showed Enhanced Cinnarizine Release in Hypochlorhydria/Achlorhydria Dissolution Model

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 627
Author(s):  
Ahmad A. Shahba ◽  
Ahmad Y. Tashish ◽  
Fars K. Alanazi ◽  
Mohsin Kazi
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Negative Impact ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Dissolution Model ◽  
Dissolution Efficiency ◽  
Drug Free

The study aims to design a novel combination of drug-free solid self-nanoemulsifying drug delivery systems (S-SNEDDS) + solid dispersion (SD) to enhance cinnarizine (CN) dissolution at high pH environment caused by hypochlorhydria/achlorhydria. Drug-loaded and drug-free liquid SNEDDS were solidified using Neusilin® US2 at 1:1 and 1:2 ratios. Various CN-SDs were prepared using freeze drying and microwave technologies. The developed SDs were characterized by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRD). In-vitro dissolution studies were conducted to evaluate CN formulations at pH 6.8. Drug-free S-SNEDDSs showed acceptable self-emulsification and powder flow properties. DSC and XRD showed that CN was successfully amorphized into SDs. The combination of drug-free S-SNEDDS + pure CN showed negligible drug dissolution due to poor CN migration into the formed nanoemulsion droplets. CN-SDs and drug-loaded S-SNEDDS showed only 4% and 23% dissolution efficiency (DE) while (drug-free S-SNEDDS + FD-SD) combination showed 880% and 160% enhancement of total drug release compared to uncombined SD and drug-loaded S-SNEDDS, respectively. (Drug-free S-SNEDDS + SD) combination offer a potential approach to overcome the negative impact of hypochlorhydria/achlorhydria on drug absorption by enhancing dissolution at elevated pH environments. In addition, the systems minimize the adverse effect of adsorbent on drug release.

scholarly journals Actively Targeted and Redox Responsive Delivery of Anticancer Drug by Chitosan Nanoparticles

Pharmaceutics ◽  
2019 ◽  
Vol 12 (1) ◽  
pp. 26 ◽  
Author(s):  
Elisabetta Mazzotta ◽  
Selene De Benedittis ◽  
Antonio Qualtieri ◽  
Rita Muzzalupo
Keyword(s):  
Drug Release ◽  
Cancer Cells ◽  
Anticancer Drug ◽  
Water Solubility ◽  
Chitosan Nanoparticles ◽  
Controlled Drug Release ◽  
Dependent Manner ◽  
High Concentration ◽  
Redox Responsive

The clinical efficacy of methotrexate (MTX) is limited by its poor water solubility, its low bioavailability, and the development of resistance in cancer cells. Herein, we developed novel folate redox-responsive chitosan (FTC) nanoparticles for intracellular MTX delivery. l-Cysteine and folic acid molecules were selected to be covalently linked to chitosan in order to confer it redox responsiveness and active targeting of folate receptors (FRs). NPs based on these novel polymers could possess tumor specificity and a controlled drug release due to the overexpression of FRs and high concentration of reductive agents in the microenvironment of cancer cells. Nanoparticles (NPs) were prepared using an ionotropic gelation technique and characterized in terms of size, morphology, and loading capacity. In vitro drug release profiles exhibited a glutathione (GSH) dependence. In the normal physiological environment, NPs maintained good stability, whereas, in a reducing environment similar to tumor cells, the encapsulated MTX was promptly released. The anticancer activity of MTX-loaded FTC-NPs was also studied by incubating HeLa cells with formulations for various time and concentration intervals. A significant reduction in viability was observed in a dose- and time-dependent manner. In particular, FTC-NPs showed a better inhibition effect on HeLa cancer cell proliferation compared to non-target chitosan-based NPs used as control. The selective cellular uptake of FTC-NPs via FRs was evaluated and confirmed by fluorescence microscopy. Overall, the designed NPs provide an attractive strategy and potential platform for efficient intracellular anticancer drug delivery.

Formulation and Evaluation of Trilayered Tablets of Zolmitriptan

2016 ◽  
Vol 9 (6) ◽  
pp. 3512-3523
Author(s):  
Abdul Saleem Mohammad ◽  
Seema Farheen ◽  
Nuha Rasheed
Keyword(s):  
Drug Release ◽  
Polymer Concentration ◽  
Controlled Drug Release ◽  
In Vitro Dissolution ◽  
Compression Method ◽  
First Order ◽  
First Order Kinetics ◽  
Ftir Studies ◽  
Evaluation Parameters

The present study outlines a systematic approach to formulate and evaluate trilayered tablets of zolmitriptan by geomatrix technology by using different concentrations of HPMC, xanthangum and ethyl cellulose by direct compression method for controlled release, which may produce the controlled drug release in the treatment of migraine disorder. The different release rates from these formulations were obtained from in vitro dissolution studies. From the results it was observed that the release rate was greatly influenced by the polymer concentration. In order to obtain a formulation which releases more than 90% of drug within 12-14hrs, sixteen formulation trials of the active layer have been prepared and the drug release follows first order kinetics. Hence, the formulation trial F14  showed about 99% drug release in 12 hrs, where the drug release was dependent on concentration of drug in tablets  and showed various physiochemical evaluation parameters like hardness, thickness and also showed  drug excipient compatibilities by DSC and FTIR studies. 

Transdermal patch, co-loaded with Pregabalin and Ketoprofen for improved bioavailability; in vitro studies

2021 ◽  
pp. 096739112110045
Author(s):  
Nida Shafique ◽  
Tuba Siddiqui ◽  
Muhammad Zaman ◽  
Zoya Iqbal ◽  
Shahid Rasool ◽  
...  
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
Controlled Drug Release ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Transdermal Drug Delivery System ◽  
Hydrophobic Polymers ◽  
The Matrix ◽  
Permeation Studies

The current study was aimed to fabricate a transdermal drug delivery system (TDDS) containing Ketoprofen (KTF) and Pregabalin (PGB) for controlled drug release, avoidance of the first-pass metabolism, and increased patient compliance. TDDS of KTF and PGB were formulated using the solvent casting method. Various ratios of hydrophilic polymer (HPMC) and hydrophobic polymers (Eudragit L-100 and Ethyl Cellulose) were employed for the formulation of transdermal patches. PG and oleic acid were used as a permeation enhancer, and PEG-400 was employed as a plasticizer. Surface morphology has confirmed the uniform distribution of drugs throughout the matrix and the excellent compatibility of the selected ingredients. All the formulation showed folding endurance of more than 300, which exhibited that all patches have suitable mechanical strength. One hundred percent flatness also showed good stability of the patches and suitability of the selected ingredients. In vitro drug permeation studies showed more than 97% and 95% release of PGB and KTF, respectively, during the in vitro dissolution studies. The drug release mechanism investigated with various kinetic models exhibited that the rate of drug release was not dependent on initial concentrations of the drug present in the patches and was following the drug diffusion mechanism.

scholarly journals FORMULATION AND EVALUATION OF TELMISARTAN FAST DISSOLVING TABLETS USING JACK FRUIT SEED STARCH AS SUPERDISINTEGRANT

2019 ◽  
pp. 25-32
Author(s):  
SUNDEEP MUPPARAJU ◽  
VIDYADHARA SURYADEVARA ◽  
SANDEEP DOPPALAPUDI ◽  
SASIDHAR REDDYVALLAM L. C. ◽  
RAMU ANNE ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Hydroxide ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Stability Studies ◽  
Scanning Calorimetry ◽  
Accelerated Stability ◽  
Jack Fruit Seed ◽  
Croscarmellose Sodium

Objective: The main objective of the current study is to enhance the solubility of Biopharmaceutical Classification System (BCS) Class-II drug Telmisartan using jack fruit seed starch as super disintegrant which increases drug release. Methods: Starches were extracted using alkali technique using sodium hydroxide at 0.1%, 0.25%, and 0.5% concentrations and water from Jack fruit seed powder. These starches were evaluated for various phytochemical and physicochemical tests. Fast dissolving tablets were prepared using Telmisartan, jack fruit seed starch and Croscarmellose sodium in various concentrations using wet granulation technique. Various pre and post-compression parameters were evaluated along with in vitro drug release studies, characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD) and accelerated stability studies. Results: Phytochemical tests revealed the presence of only starch in all the extracts. The starch prepared from 0.1% sodium hydroxide (JFS2) showed best physicochemical properties. From in vitro dissolution studies, it was observed that formulations F5 and F11 containing 15% w/w of JFS2 and 15% w/w of croscarmellose sodium showed faster disintegration and increased dissolution rate compared with other formulations. FTIR and DSC studies showed that there were no major interactions among drug and excipients. XRD studies revealed the nature of formulations. Accelerated stability studies revealed the stability of tablets. Conclusion: Thus, the tablets prepared using Jack fruit seed starch revealed the super disintegrant property of starch.

scholarly journals PREPARATION AND EVALUATION OF DOLUTEGRAVIR SOLID DISPERSIONS

2021 ◽  
pp. 193-198
Author(s):  
SUNDEEP MUPPARAJU ◽  
VIDYADHARA SURYADEVARA ◽  
SANDEEP DOPPALAPUDI
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Content Uniformity ◽  
Fusion Method ◽  
Scanning Calorimetry ◽  
Poloxamer 188

Objective: The current work mainly focuses on solubility enhancement of dolutegravir which is a BCS (Biopharmaceutical Classification System) class-II drug using various excipients. Methods: Solid dispersions of dolutegravir were prepared by solvent evaporation and fusion methods using carriers like poloxamer-188 and plasdone K-29/32 in different ratios (1:0.5 to 1:3.0). The amount of dolutegravir used was kept constant and the polymer concentrations were increased. Various physical parameters like angle of repose, carr’s index, Hausner’s ratio were calculated for the prepared solid dispersions. They were also evaluated for particle size and drug content uniformity along with in vitro drug release. Characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM) and X-Ray Diffraction (XRD) were also done. Results: Dolutegravir solid dispersions showed good to excellent flow properties. From in vitro dissolution studies, it was observed that the solid dispersion formulation DF3 containing dolutegravir and poloxamer-188 in 1:1.5 ratios prepared by fusion method showed better dissolution rate when compared with other formulations. The dissolution parameters were also evaluated. DF3 showed a higher drug release of 86.33% in 60 min. FTIR and DSC studies revealed that there were no major interactions between drug and excipients. XRD studies revealed the nature of formulations. Conclusion: The solid dispersions prepared using poloxamer-188 by fusion method has enhanced the solubility of dolutegravir.

Formulation and Evaluation of Orally Disintegrating Tablets of Lamotrigine

2015 ◽  
Vol 8 (2) ◽  
pp. 2881-2888
Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
P Karade
Keyword(s):  
Drug Release ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Orally Disintegrating Tablet ◽  
Drug Content ◽  
Weight Variation ◽  
Wetting Time ◽  
Croscarmellose Sodium

The aim of this study was to design orally disintegrating tablet (ODT) of Lamotrigine. It is an Antiepileptic drug which is widely used in epilepsy. It is also used in simple and complex partial seizures and secondary generalized tonic-clonic seizures. It is poorly water soluble drug (0.46 mg/ml). Thus, an attempt was made to enhance the water solubility by complexation with β-cyclodextrin (1:1 molar ratios). The orally disintegrating tablet of lamotrigine was prepared by direct compression method using different concentration of superdisintegrants such as Sodium starch glycollate, croscarmellose sodium by sublimating agent such as camphor. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies. The prepared tablets were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. The disintegration time for the complexed tablets prepared by different concentration of superdisintegrants was found to be in range of 32.54 ± 0.50 to 55.12 ± 0.57 sec and wetting time of the formulations was found to be in range of 28.47 ± 0.67 to 52.19 ± 0.72 sec. All the formulation showed almost 100 percent of drug release within 15 min. Among all the formulation F6 and F7 prepared with 18% croscarmellose sodium and camphor shows faster drug release, respectively 10 min, F6 gives good result for disintegration time, drug release, wetting time and friability. Further formulations were subjected to stability testing for 30 days at temperature of 40 ± 5 ºC/75 ± 5 %RH. Tablets showed no appreciable changes with respect to physical appearance, drug content, disintegration time and dissolution profiles. Results were statistically analyzed by one-way ANOVA at a p < 0.05. It was found that, the data at any point of time are significant at p < 0.05.

Sign in / Sign up

Export Citation Format

Share Document