scholarly journals Formulation and Characterization of Chitosan Based Dexibuprofen Nanoparticles Using Ionotropic Gelation Method

2021 ◽  
Vol 11 (6) ◽  
pp. 48-57
Author(s):  
Vivekanandan S. ◽  
Lindholm Berit ◽  
.Raghunandan Reddy K ◽  
Venkatesan P.
Keyword(s):  
Drug Release ◽  
Sodium Tripolyphosphate ◽  
Inflammatory Cells ◽  
Ionotropic Gelation ◽  
Control Drug ◽  
Racemic Ibuprofen ◽  
Ft Ir ◽  
Nanoparticle Formulation ◽  
Pharmacologically Active

Dexibuprofen is a pharmacologically active enantiomer of racemic ibuprofen (NSAID), which is used to treat pain and inflammation. Like common NSAIDs, Dexibuprofen is an active enantiomer of ibuprofen that suppresses the prostanoid synthesis in the inflammatory cells via inhibition of the COX-2 isoform of the arachidonic acid COX. The therapeutic use of Dexibuprofen is limited by the rapidity of the onset of its action and its short biological half-life. Hence, our aim was to develop Dexibuprofen nanoparticles formulation to overcome these disadvantages using optimized concentration of polymers by appropriate methods for nanoparticle preparation. The drug and the nanoparticle formulation of Dexibuprofen F11 were comparatively assessed for FT IR spectrums by using FT-IR method. The DSC study was used as one of the tool to assess the compatibility between drug and the excipients. As per DSC thermograms, the drug as well as drug with mixture of excipients chitosan, sodium tripolyphosphate had shown no interactions with dexibuprofen. The ionotropic gelation method was used to prepare Dexibuprofen nanoparticles. The chitosan and sodium tripolyphosphate (TPP) of different concentrations were used as polymers to prepare Dexibuprofen nanoparticles. Total eleven different formulations were explored with different concentrations of drug : polymer ratios using ionotropic gelation method to identify optimal concentrations of polymer. Among different formulations, F11 formulation with optimized concentration of 5% chitosan and 1% Sodium tripolyphosphate polymers along with Dexibuprofen showed maximum drug release. The objective was to evaluate the developed Dexibuprofen nanoparticles. In-vitro drug release was evaluated in 0.05M phosphate buffer pH7.2 and found that the drug release of F11 formulation of Dexibuprofen nanoparticle had shown release till 24 hours more than that of other trials. Hence, F11 formulation was considered as the optimized nanoparticle formulation to control drug release till 24 hours. The entrapment efficacy of the formulated Nanoparticles was found to be in the range of 75.48%-91.22% respectively.

Characterization and Screening of a Novel Multiparticulate Pulsatile Delivery of Aceclofenac

2016 ◽  
Vol 9 (5) ◽  
pp. 3494-3501
Author(s):  
Bipul Nath ◽  
Santimoni Saikia
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Alginate Beads ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Ft Ir ◽  
Lag Period ◽  
Pulsatile Delivery ◽  
Ca Alginate

In the present investigation, sodium alginate based multiparticulate system overcoated with time and pH dependent polymer was studied in the form of oral pulsatile system to achieve pulsatile with sustained release of aceclofenac for chronotherapy of rheumatoid arthritis seven batches of micro beads with varying concentration of sodium alginate (2-5 %) were prepared by ionotropic-gelation method using CaCl2 as cross-linking agent. The prepared Ca-alginate beads were coated with 5% Eudragit L100 and filled into pulsatile capsule with varying proportion of plugging materials. Drug loaded microbeads were investigated for physicochemical properties and drug release characteristics. The mean particle sizes of drug-loaded microbeads were found to be in the range 596±1.1 to 860 ± 1.2 micron and %DEE in the range of 65-85%. FT-IR and DSC studies revealed the absence of drug polymer interactions. The release of aceclofenac from formulations F1 to F7 in buffer media (pH 6.8) at the end of 5h was 65.6, 60.7, 55.7, 41.2, 39.2, 27 and 25% respectively. Pulsatile system filled with eudragit coated Ca-alginate microbeads (F2) showed better drug content, particle size, surface topography, in-vitro drug release in a controlled manner. Different plugging materials like Sterculia gum, HPMC K4M and Carbopol were used in the design of pulsatile capsule. The pulsatile system remained intact in buffer pH 1.2 for 2 hours due to enteric coat of the system with HPMCP. The enteric coat dissolved when the pH of medium was changed to 7.4. The pulsatile system developed with Sterculia gum as plugging material showed satisfactory lag period when compared to HPMC and Carbopol.

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.

AN ENHANCEMENT OF SOLUBILITY OF PIOGLITAZONE HYDROCHLORIDE USING LIQUISOLID TECHNIQUE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (06) ◽  
pp. 36-39
Author(s):  
S Deshmane ◽  
◽  
K Gandhi ◽  
S. Nagpure ◽  
A. Sawant ◽  
...  
Keyword(s):  
Mathematical Model ◽  
Drug Release ◽  
Dissolution Rate ◽  
In Vivo Study ◽  
Dimethyl Acetamide ◽  
Volatile Liquid ◽  
Ft Ir ◽  
Ir Study

The new mathematical model was developed by studying angle of slide using N, N-dimethyl acetamide, non-volatile liquid vehicle and prepared liquisolid tablets, in which the different concentrations of non-volatile liquid adsorbed over carrier and coating material separately. Both DSC and FT-IR study showed better compatibility and stability. The optimized formulation showed higher drug release during in-vitro and in-vivo study against conventional and marketed preparation. The present work concludes that N, N-dimethyl acetamide enhanced the solubility of pioglitazone HCl with higher dissolution rate through liquisolid technique.

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 characterization of flurbiprofen loaded microsponge based gel for sustained drug delivery

2019 ◽  
Vol 10 (4) ◽  
pp. 2765-2776
Author(s):  
Naresh Kshirasagar ◽  
Goverdhan Puchchakayala ◽  
Balamurgan K
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Diffusion Method ◽  
Skin Delivery ◽  
Sustained Action ◽  
Release Studies ◽  
Ft Ir ◽  
Polymer Ratio

The new investigation in this present work is to develop microsponges constructed novel drug delivery system for sustained action of Flurbiprofen. Quai-emulsion solvent diffusion method was engaged using Ethyl cellulose and Eudragit RS100 with drug: polymer ratio for development of microsponges. For optimization purposes, several factors are considered in the investigation. Several evaluation studies for the formed microsponges were carried out FT-IR, SEM, DSC, X-RD, particle size analysis, morphology, drug loading and In vitro drug release studies were carried out. Finally, it was concluded that there is no drug-polymer interaction as per DSC & FT-IR. Encapsulation efficiency, particle size and drug content showed a higher impact on alteration of drug-polymer ratio. SEM studies showed that morphological microsponges are spherical and porous in nature and with the mean particle size of 38.86 μm. The gel loaded with microsponges, were followed by In vitro and Ex vivo drug release studies by modified Franz diffusion cell. Skin delivery of optimized formulation enhanced the drug residence time and maintained therapeutic concentration for an extended period of time, which is possible to show sustained action of the drug.

scholarly journals Synthesis, structural characterization, cytotoxicity and encapsulation studies of N,Nʹ-(1, 2-dicyano-1,2-vinylene)-bis(4-hydroxysalicylideneaminato) di(p-chlorobenzyl)tin as potential anticancer drug

2019 ◽  
Vol 42 (1) ◽  
pp. 94-101
Author(s):  
Nur Adibah Mohd Amin ◽  
Rusnah Syahila Duali Hussen ◽  
See Mun Lee ◽  
Kae Shin Sim ◽  
Suerialoasan Navanesan
Keyword(s):  
Drug Release ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Spherical Shape ◽  
Average Diameter ◽  
Diphenyltetrazolium Bromide ◽  
Ft Ir ◽  
Phosphate Buffered Saline ◽  
Mcf 7

Abstract Two new diorganotin(IV) complexes with the general formula (RC7H6)2Sn(L) (where RC7H6 = p-ClBn, C1; and p-FBn, C2) were prepared based on the reaction of 2,3-bis(4-hydroxysalicylidene-amino)-maleic nitrile (L) with substituted dibenzyltin(IV) dichloride. The structures were confirmed by elemental analysis, Fourier transform infrared (FT-IR), proton and carbon nuclear magnetic resonance (1H and 13C NMR). They were tested against several cancer cell lines by using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. C1, which was most effective against MCF-7 breast cancer cell line, was further investigated in formulation and encapsulation studies, including drug encapsulation efficiency, particle size, morphology and in vitro drug release. An encapsulation of about 90% was achieved with particles of 128 nm average diameter. Field emission scanning electron microscopy (FESEM) confirmed a spherical shape for the encapsulated C1. The cumulative drug release over a period of 60 days in phosphate buffered saline (PBS) at pH 7.4 was 75%. Based on these results, the formulated drug has the potential of a slow release drug for cancer chemotherapy.

scholarly journals Chitosan-based nanoparticles sustenance and potentiation of the antibacterial effect of ampicillin against drug resistance among strains of Escherichia coli

Bio-Research ◽  
2020 ◽  
Vol 18 (2) ◽  
Author(s):  
EB Onuigbo ◽  
C Anozie-Ikeanyi ◽  
NE Edeh ◽  
CO Eze ◽  
TH Gugu
Keyword(s):  
Drug Resistance ◽  
Drug Release ◽  
Encapsulation Efficiency ◽  
Antibacterial Effect ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
In Vitro Drug Release ◽  
E Coli ◽  
Ampicillin Trihydrate

The study seeks to evaluate nanoparticles based on chitosan for enhanced delivery of ampicillin in plasmid-mediated drug resistance. Serial dilutions of a mixed population of E. coli was plated on nutrient agar and streaked on Replica-plate 25 random colonies using MacConkey agar with or without ampicillin (100 µg/ml) daily for 96 h. Nanoparticles were prepared by cross-linking chitosan with sodium tripolyphosphate with ampicillin trihydrate adsorbed. Three different batches were prepared for optimization. The nanoparticles were optimized based on encapsulation efficiency, in vitro drug release, pH stability and microbiological assay using two laboratory strains of E. coli. Increased resistance to ampicillin due to possible plasmid transfer was established in vitro after 96 h. The encapsulation efficiency of the three batches was between 21-57 %. The drug release showed a burst effect and slow extended release over 8 h and reached a peak of about 19 % release at the 6 and 7 h in Batch A, B and C. The pH of the particles was stable over a period of 6 d. The nanoparticles containing only 0.075 mg of ampicillin dropped in an agar well plate inoculated with 1 ml of E. coli J62 lac pro trp hispFlac::Tn3 (AmpR) gave an IZD of ≥ 25 mm. Chitosan nanoparticles holds good potentials in potentiating the antibacterial effect of ampicillin against possible plasmid-mediated drug resistance

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.

scholarly journals Silk fibroin/polyethylene glycol nanofibrous membranes loaded with curcumin

2017 ◽  
Vol 21 (4) ◽  
pp. 1587-1594 ◽  
Author(s):  
Qing Liu ◽  
Shufa Zhou ◽  
Zeyu Zhao ◽  
Ting Wu ◽  
Rong Wang ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Drug Release ◽  
Silk Fibroin ◽  
Drug Loading ◽  
Control Drug ◽  
Nanofiber Membranes ◽  
Utilization Ratio ◽  
The Stability ◽  
Control Drug Release

In order to improve the stability, utilization ratio and anti-tumor effect of curcumin drug, a set of curcumin-loaded nanofiber membranes with drug releasing property were fabricated using silk fibroin and polyethylene glycol. Various curcumin-loaded silk fibroin nanofiber membranes with different components and drug loading percentages were prepared using electrospinning technology. The morphology structure, mechanical properties, secondary structure, drug release property in vitro, and their interaction effects of the curcumin-loaded silk fibroin nanofiber membranes were examined. The result of in-vitro drug release experiment showed that the curcumin can be released stably up to 350 hours, the drug releasing speed increased with the decrease of the diameter of the fibers. The stability and utilization ratio of curcumin was improved after loading with curcumin-loaded silk fibroin nanofiber membranes. In conclusion, it can be used as a control drug release system alternately in the future.

scholarly journals Formulate and evaluate once daily sustained release tablet of highly soluble drug of metformin HCL

2020 ◽  
Vol 1 (4) ◽  
pp. 138-145
Author(s):  
B. Valli Manalan ◽  
Nadendla Swathi ◽  
Narra Nandini ◽  
N. Hari Sree ◽  
Nilla Tejaswi Sai Maha Lakshmi ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Stability Studies ◽  
Chemical Changes ◽  
Accelerated Stability ◽  
The Matrix ◽  
Ft Ir

The aim of the present study was to design an oral sustained release matrix tablet of highly water soluble biguanide anti diabetic drug. The matrix tablets are prepared by melt granulation method using HPMC K 200M as hydrophilic drug release retarding polymer, and stearic acid as melt able binder as well as hydrophobic carrier. The drug and excipients compatibility was studied by FT – IR. The formulated matrix tablets were characterized for physical parameters and in vitro dissolution profile. FT – IR spectra revealed the absence of drug excipients interaction. The physical parameters of the tablets were found within the limits. The drug release kinetics demonstrated that by increasing the concentration of hydrophilic polymer and hydrophobic carrier the drug release rate was retarded proportionally. Kinetic modelling of in vitro release profile revealing that the drug release from the matrix tablets following first order kinetics, and the drug release mechanism of optimized (F7) formula following non fickian transport mechanism. Accelerated stability studies were performed according to ICH guide lines. Temperature 40±20 c and relative humidity 75±5% RH to study physical and chemical changes of formulation. No physical or chemical changes were observed after t accelerated stability studies.

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