The Development of Pemetrexed Diacid-Loaded Gelatin-Cloisite 30B (MMT) Nanocomposite for Improved Oral Efficacy Against Cancer: Characterization, In-Vitro and Ex-Vivo Assessment

2020 ◽  
Vol 17 (3) ◽  
pp. 246-256
Author(s):  
Kriti Soni ◽  
Ali Mujtaba ◽  
Md. Habban Akhter ◽  
Kanchan Kohli
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Confocal Laser ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Cloisite 30B ◽  
Ft Ir

Aim: The intention of this investigation was to develop Pemetrexed Diacid (PTX)-loaded gelatine-cloisite 30B (MMT) nanocomposite for the potential oral delivery of PTX and the in vitro, and ex vivo assessment. Background: Gelatin/Cloisite 30 B (MMT) nanocomposites were prepared by blending gelatin with MMT in aqueous solution. Methods: PTX was incorporated into the nanocomposite preparation. The nanocomposites were investigated by Fourier Transmission Infra Red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscope (SEM) X-Ray Diffraction (XRD) and Confocal Laser Microscopy (CLSM). FT-IR of nanocomposite showed the disappearance of all major peaks which corroborated the formation of nanocomposites. The nanocomposites were found to have a particle size of 121.9 ± 1.85 nm and zeta potential -12.1 ± 0.63 mV. DSC thermogram of drug loaded nanocomposites indicated peak at 117.165 oC and 205.816 oC, which clearly revealed that the drug has been incorporated into the nanocomposite because of cross-linking of cloisite 30 B and gelatin in the presence of glutaraldehyde. Results: SEM images of gelatin show a network like structure which disappears in the nanocomposite. The kinetics of the drug release was studied in order to ascertain the type of release mechanism. The drug release from nanocomposites was in a controlled manner, followed by first-order kinetics and the drug release mechanism was found to be of Fickian type. Conclusion: Ex vivo gut permeation studies revealed 4 times enhancement in the permeation of drug present in the nanocomposite as compared to plain drug solution and were further affirmed by CLSM. Thus, gelatin/(MMT) nanocomposite could be promising for the oral delivery of PTX in cancer therapy and future prospects for the industrial pharmacy.

Preparation, characterizations and in vitro evaluation of Econazole-Btamethasone loaded solid lipid nanoparticles (SLNs)

2021 ◽  
pp. 1-12
Author(s):  
Kamran Khan ◽  
Shefaat Ullah Shah ◽  
Yusuf S. Althobaithi ◽  
Kifayat Ullah Shah ◽  
Aman Ullah ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Side Effects ◽  
Drug Release ◽  
Oral Delivery ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
Ex Vivo ◽  
Sem Images ◽  
Drug Content

Tremendous increase of fungal infections in hospitalized or immune compromised patients has been reported from the last two decades. These infections are commonly treated using econazole and miconazole that have shorter half-life and produce severe side effects. All such issues can be addressed using targeted drug delivery. We developed SNLs based formulation for the treatment of mycosis. The high pressure homogenization method was employed for formulation followed by characterization, assay for antifungal activity, in vitro drug release and ex vivo permeation. The particle size of Econazole-Betamethasone-loaded SLNs, Econazole-loaded SLNs, Betamethasone-loaded SLNs and Blank SLNs were 377.4±23 nm, 298.7±9 nm, 177.7±15 nm and 113.4±6 nm respectively. The SEM images displayed that droplets are uniform and spherical in shape which ranged from 113.4±6 to 377.4±23 nm. In DSC, the SLNs formulation showed endothermic peak at 185.2 °C±0.9. Drug content of Econazole loaded SLNs was 82±0.1 and its entrapment efficiency was approximately 90.4±0.2. Betamethasone SLNs displayed highest drug content which was 83.5±0.4 while encapsulation efficiency of same formulation was 94.2±0.4. The Econazole and Betamethasone combined SLNs exhibited drug content of 80±0.3 while its encapsulation efficiency was 93.1±0.5. E-SLNs have significantly high drug release (p <  0.05) as compared to other formulation B-SLNs and EB-SLNs.The Econazole loaded formulations displayed antifungal activity with no synergistic or antagonistic effect with each other. Drug permeation from Econazole SLNs, Betamethasone SLNs and combined Econazole and Betamethasone SLNs was 45%, 40% and 38% respectively. Overall, SLN’s are an effective carrier for topical delivery of antifungals agents and that may be helpful in bypassing the serious side effects associated with oral delivery.

Synthesis and characterization of Chitosan-Catechol conjugates: Development and in vitro, in silico and in vivo evaluation of mucoadhesive pellets of lafutidine

2021 ◽  
pp. 088391152199784
Author(s):  
Loveleen Kaur ◽  
Ajay Kumar Thakur ◽  
Pradeep Kumar ◽  
Inderbir Singh
Keyword(s):  
Drug Release ◽  
In Silico ◽  
Ex Vivo ◽  
Strong Interactions ◽  
Dissolution Time ◽  
Sem Images ◽  
In Vivo Evaluation ◽  
Release Studies

Present study was aimed to synthesize and characterize Chitosan-Catechol conjugates and to design and develop mucoadhesive pellets loaded with lafutidine. SEM images indicated the presence of fibrous structures responsible for enhanced mucoadhesive potential of Chitosan-Catechol conjugates. Thermodynamic stability and amorphous nature of conjugates was confirmed by DSC and XRD studies respectively. Rheological studies were used to evaluate polymer mucin interactions wherein strong interactions between Chitosan-Catechol conjugate and mucin was observed in comparison to pristine chitosan and mucin. The mucoadhesion potential of Chitosan-Catechol (Cht-C) versus Chitosan (Cht) was assessed in silico using molecular mechanics simulations and the results obtained were compared with the in vitro and ex vivo results. Cht-C/mucin demonstrated much higher energy stabilization (∆E ≈ −65 kcal/mol) as compared to Cht/mucin molecular complex. Lafutidine-loaded pellets were prepared from Chitosan (LPC) and Chitosan-Catechol conjugates (LPCC) and were evaluated for various physical properties viz. flow, circularity, roundness, friability, drug content, particle size and percent mucoadhesion. In vitro drug release studies on LPC and LPCC pellets were performed for computing t50%, t90% and mean dissolution time. The values of release exponent from Korsmeyer-Peppas model was reported to be 0.443 and 0.759 for LPC and LPCC pellets suggesting Fickian and non-Fickian mechanism representing drug release, respectively. In vivo results depicted significant controlled release and enhanced residence of the drug after being released from the chitosan-catechol coated pellets. Chitosan-Catechol conjugates were found to be a promising biooadhesive polymer for the development of various mucoadhesive formulations.

scholarly journals Eudragit S-100 coated sodium alginate microspheres of naproxen sodium: Formulation, optimization and in vitro evaluation / Alginatne mikrosfere naproksen natrija obložene Eudragitom S-100: Priprava, optimizacija i in vitro vrednovanje

2012 ◽  
Vol 62 (4) ◽  
pp. 529-545 ◽  
Author(s):  
Anuj Chawla ◽  
Pooja Sharma ◽  
Pravin Pawar
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Naproxen Sodium ◽  
Drug Loading ◽  
Size Analysis ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
S 100 ◽  
Eudragit S 100

The aim of the study was to prepare site specific drug delivery of naproxen sodium using sodium alginate and Eudragit S-100 as a mucoadhesive and pH-sensitive polymer, respectively. Core microspheres of alginate were prepared by a modified emulsification method followed by cross-linking with CaCl2, which was further coated with the pH dependent polymer Eudragit S-100 (2.5 or 5 %) to prevent drug release in the upper gastrointestinal environment. Microspheres were characterized by FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and evaluated by scanning electron microscopy, particle size analysis, drug loading efficiency, in vitro mucoadhesive time study and in vitro drug release study in different simulated gastric fluids. Stability studies of the optimized formulation were carried out for 6 months. SEM images revealed that the surface morphology was rough and smooth for core and coated microspheres, respectively. Core microspheres showed better mucoadhesion compared to coated microspheres when applied to the mucosal surface of freshly excised goat colon. The optimized batch of core microspheres and coated microspheres exhibited 98.42 ± 0.96 and 95.58 ± 0.74 % drug release, respectively. Drug release from all sodium alginate microsphere formulations followed Higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the Korsmeyer-Peppas equation with a Fickian kinetics mechanism. Stability study suggested that the degradation rate constant of microspheres was minimal, indicating 2 years shelf life of the formulation.

scholarly journals CHEMICAL MODIFICATION, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE POTENTIALITY OF ASSAM BORA RICE STARCH

2017 ◽  
Vol 9 (9) ◽  
pp. 132 ◽  
Author(s):  
Abdul Baquee Ahmed ◽  
Iman Bhaduri
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Chemical Modification ◽  
Ex Vivo ◽  
Rice Starch ◽  
Modified Starch ◽  
Native Starch ◽  
Ft Ir

Objective: The objective of the present study was to chemical modification, characterization and evaluation of mucoadhesive potentiality of Assam bora rice starch as potential excipients in the sustained release drug delivery system. Methods: The starch was isolated from Assam bora rice and esterified using thioglycolic acid and characterized by Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC) and Nuclear magnetic resonance (NMR). The 10% w/v gel formulation based on modified bora rice starch loaded with irinotecan (0.6%) was prepared and evaluated for various rheological properties, ex-vivo mucoadhesion using goat intestine and in vitro drug release study in phosphate buffer pH 6.8.Results: The chemical modification was confirmed by FT-IR and NMR studies with the presence of the peak at 2626.74 cm-1 and a singlet at 2.51 respectively due to–SH group. Ex-vivo mucoadhesion studies showed 6.6 fold increases in mucoadhesion of the modified starch with compared to native starch (46.3±6.79g for native starch; 308.7±95.31g for modified starch). In vitro study showed 89.12±0.84 % of drug release after 6 h in phosphate buffer pH 6.8 and the release kinetics followed Non-Fickian diffusion.Conclusion: The modified Assam bora rice starch enhanced a mucoadhesive property of the native starch and thus, can be explored in future as a potential excipient for the sustained release mucoadhesive drug delivery system.

scholarly journals FORMULATION AND EVALUATION OF FLOATING-MUCOADHESIVE MICROSPHERES OF NOVEL NATURAL POLYSACCHARIDE FOR SITE SPECIFIC DELIVERY OF RANITIDINE HYDROCHLORIDE

2017 ◽  
Vol 9 (3) ◽  
pp. 15
Author(s):  
Vikram Kumar Sahu ◽  
Nitin Sharma ◽  
Pratap Kumar Sahu ◽  
Shubhini A. Saraf
Keyword(s):  
Drug Release ◽  
Drug Stability ◽  
Compatibility Study ◽  
Chemical Crosslinking ◽  
Drug Bioavailability ◽  
Sem Images ◽  
Ranitidine Hydrochloride ◽  
Plant Polysaccharide ◽  
Ft Ir

Objective: Localization of ranitidine hydrochloride (RH) into the upper part of the intestinal tract is beneficial for better drug bioavailability. Present work described the method of preparation of novel plant polysaccharide based floating microspheres for delivery of the drug into the stomach.Methods: Polysaccharide was extracted from the seeds of plant Tamarindus indica (TI). Extracted polysaccharide was evaluated for some physicochemical parameters. Floating-mucoadhesive microspheres were prepared by using extracted polysaccharide as mucoadhesive excipients while eudragit as a release controlling polymers by using emulsion crosslinking method. Chemical crosslinking was done by using epichlorohydrin. Prepared microspheres were evaluated for their drug-polymer compatibility study by using fourier transform infrared spectroscopy (FT-IR). Further characterization such as size, surface properties, swelling index, percentage encapsulation, in vitro buoyancy and drug release was performed.Results: FT-IR study confirms the chemical crosslinking of extracted polysaccharide and also drug stability during processing of microspheres. The size of microspheres was in the range of 5.38 to 7.84 µm. SEM images revealed that all batches were of spherical in size and smooth surface. The swelling index showed better swelling in the range of 158-257 percentages. Encapsulation efficiency was found to be decreased by decreasing the concentration of polysaccharide. In vitro buoyancy study possesses that formulation F1 showed better floating ability as compared to the others. Finally, in vitro drug release study revealed that prepared microspheres were able to release the 100% drug within 8-12 h, indicating sustain release behavior.Conclusion: Present study concludes that polysaccharide of TI may be used as excipients for the preparation of floating-mucoadhesive microspheres.

DESIGN AND IN VITRO EVALUATION OF MUCOADHESIVE BUCCAL FILMS OF LERCANIDIPINE HCL

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (07) ◽  
pp. 31-40
Author(s):  
H. Doddayya ◽  
◽  
S.S Patil ◽  
M Suman ◽  
P Kumar ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Zero Order Kinetics ◽  
Accelerated Stability ◽  
Buccal Films ◽  
Lercanidipine Hydrochloride

Lercanidipine hydrochloride, an anti hypertension drug, undergoes extensive first pass metabolism to inactive metabolites leading to very poor oral bioavailability. To overcome this problem, buccal films of Lercanidipine hydrochloride were prepared by solvent casting method, employing HPMC, HPC (alone and in combination with PVP) and PVP K30. The film thickness, weight, folding endurance, mucoadhesive strength and time were dependent on the nature and concentration of polymers used. The optimized film (F12, HPMC 3% and PVP 1.5%) showed: Swelling index (51.26 ± 1.90 %), ex vivo mucoadhesive strength (12.64 ± 0.83 grams) and time (3.6 ± 0.5hrs). In vitro drug release was inversely proportional to the polymeric concentration. Ex- vivo drug release studies carried out using goat buccal membrane was slower (42.90%, 6 hrs) compared to in vitro drug release (74.2%, 8hrs) for the same formulation (F12). The drug release mechanism for the optimized formulation followed zero order kinetics. FT-IR and DSC studies revealed the absence of any interaction between the formulation ingredients. The films remained stable during the accelerated stability conditions.

scholarly journals Eudragit: A Novel Carrier for Controlled Drug Delivery in Supercritical Antisolvent Coprecipitation

Polymers ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 234 ◽  
Author(s):  
Paola Franco ◽  
Iolanda De Marco
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Liquid Solution ◽  
Scanning Calorimetry ◽  
Supercritical Antisolvent ◽  
Vis Spectroscopy ◽  
Mean Size ◽  
Ft Ir ◽  
Optimized Conditions ◽  
Prolonged Drug Release

In this work, the supercritical antisolvent (SAS) process was used to coprecipitate Eudragit L100-55 (EUD) with diclofenac (DICLO) and theophylline (THEOP), with the aim of obtaining composite microparticles with a prolonged drug release for oral delivery. Working at the optimized conditions in terms of pressure and overall concentration in the liquid solution (10.0 MPa and 50 mg/mL), microparticles of EUD/DICLO 20/1 and 10/1 w/w were produced with a mean size of 2.92 µm and 1.53 µm, respectively. For the system EUD/THEOP, well-defined spherical microspheres with a mean diameter ranging from 3.75 µm and 5.93 µm were produced at 12.0 MPa. The produced composite systems were characterized by various techniques, such as scanning electron microscopy, differential scanning calorimetry, X-ray microanalysis, FT-IR and UV–vis spectroscopy. Dissolution studies showed the potential of EUD to prolong the drug release, significantly, up to a few days.

scholarly journals IN VITRO ENTRAPMENT AND RELEASE STUDIES OF LEVOFLOXACIN USING EPICHLOROHYDRIN-CROSSLINKED HYDROGEL

2019 ◽  
pp. 138-144
Author(s):  
ANGELI ANN S RESCOBER
Keyword(s):  
New Zealand ◽  
Drug Release ◽  
Release Rate ◽  
Drug Loading ◽  
Ophthalmic Solution ◽  
Antimicrobial Activities ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Polymer Ratio

Objective: This study aimed to optimize and evaluate the controlled release rate, ocular irritancy, and in vitro antimicrobial properties of levofloxacinentrapped in the epichlorohydrin-crosslinked hydrogel of sodium carboxymethyl cellulose (NaCMC) and gelatin.Materials and Methods: Various parameters such as polymer ratio, amount of crosslinker, temperature, reaction time, swelling capacity, and percentdrug loading were considered in Optimized levofloxacin hydrogel. Hydrogel preparations with higher amount of drug loaded were further analyzedto determine its in vitro drug release rate, ocular irritancy on New Zealand rabbits, and antimicrobial activities against Pseudomonas aeruginosaand Staphylococcus aureus. Optimized levofloxacin hydrogel (OLH) was then subjected to 3-month stability testing at 40 ± 2°C and 75 ± 5% relativehumidity in which samples were withdrawn at the end of each month for analysis.Results: Polymer groups with higher concentrations of NaCMC have higher swelling and drug loading capacities than those with higher gelatinconcentrations. Meanwhile, qualitative analysis using differential scanning calorimetry, Fourier-transform infrared spectroscopy, and scanningelectron microscopy verified the presence of levofloxacin in the epichlorohydrin-cross-linked hydrogel. Among the four polymer ratio, F3 was theoptimized hydrogel with drug-loaded concentration of 99.50%, which was within the acceptable assay limit of 0.5% levofloxacin solution based onUnited States Pharmacopeia monograph. It followed the Higuchi kinetic model with a drug release mechanism of super case 2 transport indicatinghydrogel swelling as a key factor for its controlled drug release. In vitro, antibacterial test against P. aeruginosa and S. aureus was sensitive to optimizedlevofloxacin hydrogel (OLH) with inhibitory diameter zones of 31.68 and 37.05 mm, respectively. Ocular irritancy test also showed that the OLH isnon-irritating on installation in the cul-de-sac of New Zealand rabbits.Conclusion: Optimized levofloxacin hydrogel was effective, non-irritating, and stable, which can be used as an alternative to conventional 0.5%levofloxacin ophthalmic solution.

Fast Dissolving Sublingual Strips: A Novel Approach for the Delivery of Isosorbide Dinitrate

2019 ◽  
Vol 25 (4) ◽  
pp. 311-318
Author(s):  
Marzieh Fathei ◽  
Mitra Alami-milani ◽  
Sara Salatin ◽  
Sharahm Sattari ◽  
Hassan Montazam ◽  
...  
Keyword(s):  
Drug Release ◽  
Isosorbide Dinitrate ◽  
Moisture Absorption ◽  
Ex Vivo ◽  
Hydroxypropyl Methylcellulose ◽  
Drug Bioavailability ◽  
Scanning Calorimetry ◽  
Surface Ph ◽  
Drug Content

Background: Isosorbide dinitrate (ISDN) is used for treating the angina attacks. In addition, oral ISDN is available in immediate and sustained release formulations and the bioavailability of ISDN is about 20-25% when taken orally. Further, the ISDN films are developed for sublingual drug delivery by improving drug bioavailability. The present study aimed to design and evaluate the physicochemical properties of the film formulation for sublingual delivery of ISDN. Methods: In the present study, sublingual films were prepared by the solvent casting technique using the hydroxypropyl methylcellulose (HPMC) polymers (i.e., 100, 150 and 200 mg) with a different drug to polymer ratios (i.e., 1:5, 1:7.5 and 1:10). Then, ISDN was evaluated for the film appearance, drug content, surface pH, mucoadhesion force, differential scanning calorimetry (DSC), in vitro drug release, and ex vivo permeability. Results: Based on the results, F3 formulation (1:10 ISDN to HPMC ratio) showed acceptable thickness (0.93 mm), weight (11.14 mg), surface pH (7.82), moisture absorption capacity (6.08%), elasticity (>200), mucoadhesion force (18.05 N/cm2), and drug content (6.22%). Furthermore, the results demonstrated that HPMC polymer improved the characteristics of the films, modified the bioadhesiveness, and finally, enhanced elasticity. However, DSC thermogram failed to show any crystalline drug substance in the films except for F1 (immediate release) and the endothermic peak of ISDN was absent in F2 and F3 films. Therefore, the drug which was entrapped into the film was in an amorphous or disturbed-crystalline phase of the molecular dispersion or dissolved in the melted polymer in the polymeric matrix. Moreover, the drug release from the films was faster compared to the tablet® (P<0.05). Conclusion: In general, the formulation of F1 was observed to be an appropriate candidate for developing the sublingual film for the remedial use.

scholarly journals DEVELOPMENT AND EVALUATION OF NANOEMULSION AS A CARRIER FOR TOPICAL DELIVERY SYSTEM BY BOX-BEHNKEN DESIGN

2018 ◽  
Vol 11 (8) ◽  
pp. 286
Author(s):  
Pallavi M Chaudhari ◽  
Madhavi A Kuchekar
Keyword(s):  
Drug Release ◽  
Ftir Spectroscopy ◽  
Ex Vivo ◽  
Topical Delivery ◽  
Homogenization Method ◽  
Permeation Rate ◽  
Scanning Calorimetry ◽  
Box Behnken Design ◽  
Globule Size

Objective: The aim of this study was to develop a nanoemulsion for topical delivery. Methods: Topical nanoemulsion was prepared by homogenization method. Box-behnken design was utilized to study the effect of oil, surfactant and Co-surfactant, on droplet size, entrapment efficiency and drug release. Nabumetone a non-steroidal anti-inflammatory drug was incorporated in castor oil with Tween 80 and Polyethylene glycol 600 to form the nanoemulsion by homogenization method. The nanoemulsion was further subjected to different evaluation parameters and ex-vivo study. The crystalline nature of drug was confirmed by powder X-ray diffraction studies. Drug-excipient compatibility was confirmed by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), respectively. Results: The average globule size of nabumetone-containing nanoemulsion decreased with decrease in concentration of oil and surfactant. Nanoemulsion was evaluated by pH, rheology, globule size, zeta potential, scanning electron microscopy, DSC, FTIR spectroscopy, and stability. In vitro drug release shows maximum 84.35% permeation rate through cellophane membrane and ex-vivo drug release shows 86.32% permeation rate through goat skin. Conclusion: Thus, the nanoemulsion formulated showed good results regarding topical delivery.

Sign in / Sign up

Export Citation Format

Share Document