FORMULATION AND EVALUATION OF NATEGLINIDE NANOSPONGES

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (02) ◽  
pp. 27-35
Author(s):  
A. A Bakliwal ◽  
◽  
D. S. Jat ◽  
S. G. Talele ◽  
A. G. Jadhav
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Synthesis Method ◽  
Ultra Sound ◽  
Size Analysis ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
Drug Content

The objective of the present study was to produce extended release nateglinide nanosponges for oral delivery. Preparation of nanosponges leads to solubility enhancement. Nateglinide is a BCS Class II drug, having low solubility. So, to increase the solubility of nateglinide it is formulated into nanosponges. Nanosponges using ethyl cellulose as a polymer and dichloromethane as a cross-linker were prepared successfully by ultra-sound assisted synthesis method. The effects of different drug: placebo ratios on the physical characteristics of the nanosponges as well as the drug content and in vitro drug release of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning and transmission electron microscopy of nanosponges showed that they were spongy in nature. The particle size was found to be in the range 46.37 - 97.23 nm out of which particle size of the optimized formulation was 51.79 nm and the drug content was found to 79.43 %. The optimized nanosponge formulations were selected for preparing nanosponge tablets for extended drug delivery by oral route. These tablets were prepared using xanthan gum and PVP K-30 and were evaluated by pre-compression and post-compression parameters. The nateglinide nanosponges tablet formulation were studied for different parameters using Design Expert Software. All formulations were evaluated for in vitro drug release analyzed according to various release kinetic models and it was found that it follows zero order release kinetics.

scholarly journals Development and Characterization of Ofloxacin & Prednisolone Loaded Nanostructured Lipid Carriers (Nlc) for Topical Route

2019 ◽  
Vol 4 (1) ◽  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Morphological Characteristics ◽  
Nanostructured Lipid Carriers ◽  
Diffusion Method ◽  
Prolonged Release ◽  
In Vitro Drug Release ◽  
Drug Content

Aim: The present study was designed to develop and characterize nanostructured lipid carriers (NLC) of Ofloxacin and Prednisolone for topical use in case of infections associated with inflammation. Materials and Methods: Ofloxacin was obtained as gift sample from Mankind Pharma Ltd, VillKyarta, P.O. Misserwal, Poonta Sahib, Sir Mour. H.P. Whereas Prednisolone was purchased from Yarrow chem., Mumbai. It was evaluated for its pre-formulation studies (organoleptic properties, melting point, solubility, compatibility, max. wavelength of absorption). NLCs were prepared through melt-emulsification followed by ultra-sonication technique. Further optimized batch of NLCs was incorporated into Gel. Formulated NLCs were evaluated in terms of morphological characteristics, particle size (Polydispersity Index), drug content, In-vitro drug release (using egg membrane), drug release kinetics (Ritger-Peppas diffusion method). Finally, gel containing NLCs was studied by physical characteristics, pH, viscosity, spreadability, drug content, In-vitro drug release and its kinetics. Results and Discussion: In pre-formulation study, drugs were found having the similar properties as described in Indian Pharmacopoeia (IP) and United States Pharmacopoeia (USP). SEM photomicrograph revealed that NLCs were spherical with more or less smooth surface; particle size 512.3-1703 nm and PDI- 0.399-0.742 (ofloxacin) and particle size 539.3-1736.7 nm and PDI- 0.335 - 0.711 (prednisolone);drug content was found in range of 56.7 - 75.6% for ofloxacin and 65.9 – 81.8% for prednisolone. NLC1 demonstrated maximum release rate with 83.37±1.70% and NLC8 73.96±0.53%.NLC6 was best fitted in Korsmeyer - peppas model as the regression coefficients were 0.960, 0.964, 0.977, 0.950, 0.980 & 0.987 respectively and prednisolone NLC 9 (0.953) and they were close to 1. Conclusion: In conclusion, the prepared NLCs had prolonged release effects with good potential for topical delivery of NLC based gel formulation of ofloxacin& prednisolone.

scholarly journals FORMULATION AND EVALUATION OF CHITOSAN NANOPARTICLES FOR IMPROVED EFFICACY OF ITRACONAZOLE ANTIFUNGAL DRUG

2018 ◽  
Vol 11 ◽  
Author(s):  
Charanteja Reddy , Y
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Chitosan Nanoparticles ◽  
Antifungal Drugs ◽  
Size Analysis ◽  
Therapeutic Drug ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Morphological Studies

Objective: The main objective of the study was to formulate and evaluate the chitosan nanoparticles to improve the therapeutic efficacy of itraconazole by loading in nanoparticle drug delivery system. Designing the formulation of the drug itraconazole prolongs the therapeutic concentration of the drug in the blood and which will lower the frequency of dosing and also improves the efficacy of the drug. Methods: Itraconazole nanoparticles are prepared by ionic gelation method; here, chitosan is used as polymer. The formulated nanoparticles are evaluated for external morphological studies by scanning electron microscope (SEM), drug content, in vitro drug release studies, as well as infrared (IR) spectral analysis. Results: The Fourier transform IR spectra show that there was no interaction between drug and polymers; hence, they are compatible. Percentage entrapment efficiency, drug content, and percentage yield were higher for F3 formulation. The particle size analysis shows that every particle in the formulations gave the range of 148–227 nm, respectively; increasing in the particle size observed with varying concentration of polymer. SEM analysis of the nanoparticles shows that all the formulations were spherical and smooth with ideal surface morphology. As the concentration of polymer, the drug release decreased proportionally. The stability studies were carried out on the optimized formulation for 2 months at 30±2°C and 60±5% RH and 40±2°C and 75±5% RH; finally, it was observed that there was no change in drug content and in vitro drug release profile even after storage at 30±2°C and 60±5% RH and 40±2°C and 75±5% RH for 2 months. Conclusion: Itraconazole is one among the most widely used antifungal drugs. Designing the formulation of drug itraconazole prolongs therapeutic drug concentration in the blood and decreases dosage frequency and also enhances the efficacy of drug.

scholarly journals EVALUATION OF STABILITY OF ROPINIROLE HYDROCHLORIDE AND PRAMIPEXOLE DIHYDROCHLORIDE MICROSPHERES AT ACCELERATED CONDITION

2018 ◽  
Vol 10 (4) ◽  
pp. 82
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
Gouranga Nandi
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Shelf Life ◽  
Stability Study ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Ropinirole Hydrochloride ◽  
Pramipexole Dihydrochloride

Objective: The objective of the present work was to conduct accelerated stability study as per international council for harmonisation (ICH) guidelines and to establish shelf life of controlled release dosage form of ropinirole hydrochloride and pramipexole dihydrochloride microspheres for a period of 6 mo.Methods: Most optimized batch of ropinirole hydrochloride and pramipexole dihydrochloride (F12 and M12 respectively) were selected and subjected to exhaustive stability testing by keeping the sample in stability oven for a period of 3 and 6 mo. Various parameters like surface morphology, particle size, drug content, in vitro drug release and shelf life were evaluated at 3 and 6 mo period. The surface morphology of the formulated microspheres was determined by scanning electron microscopy (SEM). The particle size of the microspheres was estimated by optical microscopy method. The drug content was assayed by the help of ultra-violet spectrophotometer (UV). The in vitro drug release was performed by using Paddle II type dissolution apparatus and the filtrate was analyzed by UV spectrophotometer. The shelf life of the optimized microspheres was calculated by using the rate constant value of the zero-order reaction.Results: A minor change was recorded in average particle size of F12 and M12 microspheres after storage for 6 mo. For F12 and M12, initially the particle size was 130.00 µm and 128.92 µm respectively and after 6 mo it was found to be 130.92 µm and 128.99 µm respectively. There was no change in surface morphology of F12 and M12 microspheres after 6 mo of storage. The shape of microspheres remained spherical and smooth after 6 mo. An insignificant difference of drug content was recorded after 6 mo compared to the freshly prepared formulation. For F12 and M12, 94.50% and 93.77% of the drug was present initially and after 6 mo 94.45% and 93.72% of the drug was recorded. In vitro drug release was recorded after 6 mo for F12 and M12. Initially, 97.99% and 97.69% of the drug was released till 14th hour respectively for F12 and M12. After 6 mo, 98.23% and 97.99% of the drug was released respectively. The percentage residual drug content revealed that the degradation of microspheres was low. Considering the initial percentage residual drug content as 100%, 99.94% of the drug was recorded for both F12 and M12. The shelf life for F12 and M12 was found to be 10 y 52 d and 10 y 70 d respectively which were determined by the zero-order kinetic equation.Conclusion: A more or less similar surface morphology, particle size, drug content and percent of drug release before and after stability study confirmed the stability of F12 and M12 microspheres after storage for 6 mo and prove the efficacy of the microspheres in the site-specific delivery of drugs in Parkinson’s disease.

scholarly journals The ALGINATE MICROSPHERES CONTAINING CURCUMIN: PREPARATION, CHARACTERIZATION, AND IN VITRO HUMAN HAEMOGLOBIN GLYCOSYLATION ASSAY

2019 ◽  
pp. 221-225
Author(s):  
KULKARNI AS ◽  
BHUJBAL SS
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Therapeutic Potential ◽  
Release Kinetics ◽  
Glycosylated Hemoglobin ◽  
Scanning Electron Micrographs ◽  
In Vitro Drug Release ◽  
Human Haemoglobin ◽  
Scanning Electron

Objective: The objective of the present study was to formulate, evaluate alginate microspheres of curcumin, and to investigate the inhibitory effect on glycosylated hemoglobin. Methods: All formulations were prepared by an ionotropic gelation technique using sodium alginate as a polymer and calcium chloride as a crosslinker in varying concentrations. The formulation batches (F1–F6) were evaluated for physical properties such as compatibility studies, percentage entrapment efficiency (%EE), microsphere yield, particle size, and polydispersity index. In vitro, drug release was studied and surface morphology was characterized by scanning electron microscopy. Results: The microspheres showed %EE, microsphere yield, particle size in the ranges of 44.86%–84.24%, 43.05%–81.4%, and 352–559 μm, respectively. In vitro, drug release and release kinetics showed that the developed curcumin microspheres system is a promising delivery system for controlled drug release. Scanning electron micrographs indicate porous and rough surface. The inhibitory properties of curcumin and microspheres (F4) on glycosylation formation were investigated in hemoglobin using quercetin as standard. The decreased in hemoglobin concentration after incubation of hemoglobin with a graded concentration of glucose over a specified time was used as an index for in vitro human hemoglobin glycosylation assay. Glycosylation inhibition was about 75% for standard quercetin, 60% for curcumin microspheres, and 38.74% for curcumin suspension occurred after 72 h. Conclusion: From these results, it can be concluded that curcumin in microsphere formulation has better therapeutic potential and could prove to be useful in the development of antidiabetic formulation.

scholarly journals CURCUMIN LOADED CHITOSAN NANOPARTICLES FOR TOPICAL DELIVERY: FORMULATION DESIGN, IN VITRO EVALUATION, KINETICS AND STABILITY STUDIES

2021 ◽  
Vol 10 (2) ◽  
pp. 48-52
Author(s):  
J Adlin Jino Nesalin ◽  
Preethi Raj M N
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Topical Delivery ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
In Vitro Drug Release ◽  
Topical Gel

The main objective of this research is to evaluate a new approach for the preparation of bio adhesive nanoparticles and to design an innovative topical delivery system for curcumin which is able to enhance the drug anticancer activity. Curcumin encapsulated nanoparticles were prepared by ionic gelation method. The nanoparticles were found to be discrete, spherical with free-flowing properties and evaluated for particle size analysis, shape (scanning electron microscopy), drug encapsulation efficiency, FTIR, DSC studies and in vitro release performance. The best selected nanoparticles formulation (FS5, containing drug: polymer ratio 1:5) was incorporated into gels with a bio adhesive polymer. The Nanoencapsulated topical gels were evaluated for pH, spreadability, extrudability, viscosity, in vitro drug release, drug release kinetics, bio adhesion test, accelerated stability of selected gel formulation. In vitro drug release rate for selected Nanoencapsulated bio adhesive topical gel (FS3 gel, containing 1 % w/w of drug loaded nanoparticles and 0.6 % w/w of Carbopol 934) was found to control curcumin release over 12h. The results were then compared statistically and obtained a satisfactory correlation. Thus, in conclusion preparation protocol of Nanoencapsulated topical gel study may be adopted for a successful delivery of Curcumin for topical use.

scholarly journals EMULSOMES FOR LIPOPHILIC ANTICANCER DRUG DELIVERY: DEVELOPMENT, OPTIMIZATION AND IN VITRO DRUG RELEASE KINETIC STUDY

2021 ◽  
pp. 114-121
Author(s):  
S. DUBEY ◽  
S. P. VYAS
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Particle Diameter ◽  
Release Profile ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Kinetic ◽  
In Vitro Drug Release ◽  
Solid Lipid

Objective: The objective of the present study was to formulate and characterize paclitaxel (Ptx) loaded sterically stabilized emulsomes to provide non-toxic and biocompatible carriers with high Ptx loading efficiency. Methods: Plain (P-Es) and sterically stabilized emulsomes (SS-Es) were prepared by a modified solvent evaporation method using tristearin as solid lipid and optimized for lipid to (DSPC+CHOL+DSPE-PEG)/ tristearin ratio, lipid/lipid-PEG (DSPC+CHOL/DSPE-PEG) molar ratio, solid lipid concentration, phospholipid concentration, organic to aqueous phase volume and homogenization time based on their effect particle size and entrapment efficiency. Optimized emulsomes were characterized for morphological features, in vitro drug release kinetics and protection from plasma protein. Results: The emulsomes so formed were uniform in size with a mean particle diameter of 275±5.52 and 195±6.4 nm for P-Es and SS-Es respectively. All the formulations showed pH dependent drug release with a slow and sustained release profile. Slower drug release was observed from sterically stabilized emulsomes than the plain emulsomes. The drug release profile followed the Higuchi model with the Fickian diffusion pattern. The Pegylation of emulsomes significantly reduced the in vitro protein absorption. Conclusion: The sterically stabilized emulsome can serve as a novel non-toxic platform with longer circulatory time for the delivery of Paclitaxel and other poorly water-soluble drugs as well.

scholarly journals APPLICATION OF NOVEL NATURAL POLYMER FOR CONTROLLING THE RELEASE OF FENOVERINE FROM CONTROLLED RELEASE MATRIX TABLETS

2017 ◽  
Vol 9 (2) ◽  
pp. 1 ◽  
Author(s):  
Ajit Kulkarni ◽  
Trushali Mandhare ◽  
Nagesh Aloorkar
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Natural Polymer ◽  
In Vitro Drug Release ◽  
Dissolution Studies ◽  
Drug Content

Objective: To explore a novel natural polymer, pullulan for controlling the release of fenoverine from matrix tablets and to elucidate the release kinetics of fenoverine from pullulan and HPMC matrices.Methods: In this study we formulated monolithic matrix tablets containing of fenoverine as controlled-release tablets by direct compression using pullulan, HPMC (Hydroxypropyl methyl cellulose) K4M and HPMC K100M polymers and evaluated for hardness, thickness, friability, weight variation drug content, in vitro drug release characteristics and FTIR (Fourier transform infrared spectroscopy) and DSC (Differential scanning calorimetry) study.Results: All the formulations showed compliance with pharmacopoeial standards. FTIR and DSC study indicated the absence of interaction between fenoverine and excipients. The formulation was optimized on the basis of acceptable tablet properties and in vitro drug release. The results of dissolution studies indicated that the formulation F5 [drug to polymer 1: 0.35] exhibited highest % cumulative drug release of 96.82±0.75 % at the end of 12 h. Optimised batch F5 showed super case II transport mechanism and followed zero order release kinetics. Short-term stability studies of the optimized formulation indicated that there were no significant changes observed in hardness, drug content and in vitro dissolution studies at the end of three months period. Similarity factor f2 was found to be 89, which indicated similar dissolution profiles before and after stability study.Conclusion: Based on above results we conclude that pullulan can be used as a polymer for retarding the release of drug from matrix formulations.Keywords: Pullulan, Fenoverine, Hydroxypropyl methyl cellulose, Controlled release, In vitro

DOXORUBICIN LOADED POLYCAPROLACTONE-CHITOSAN NANOSPHERES: FORMULATION, CHARACTERISATION AND IN VITRO EVALUATION

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (11) ◽  
pp. 17-23
Author(s):  
K Prakash ◽  
◽  
Y Phalguna ◽  
D. H. Narayana
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Chemical Interaction ◽  
Release Kinetics ◽  
Double Emulsion ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Ftir Studies ◽  
Release Studies

The present study was aimed to develop and evaluate polycaprolactone–chitosan nanospheres of doxorubicin hydrochloride (DXO) in different drug to polymer ratios using double-emulsion solvent evaporation and solvent diffusion methods. FTIR studies showed that there was no chemical interaction between the drug and polymers. Scanning electron microscopy showed the nanospheres having a discrete spherical structure without aggregation. Prepared nanospheres were characterized for particle size, zeta potential, entrapment efficiency and in-vitro drug release kinetics. Nanospheres showed the particle size of 700±105to770±115 nm with an entrapment efficiency of 66.23±0.11% to 93.62±0.17%. The DXO content was found 76±0.12% to 91±0.36% in several batches. In-vitro drug release studies were performed using the dialysis membrane method. All the drug loaded batches were rendered sustained release over a period of 24 h.

scholarly journals Formulation and in vitro Assessment of Eudragit L 100 and Eudragit S 100 Based Naproxen Microspheres

2016 ◽  
Vol 15 (1) ◽  
pp. 47-55
Author(s):  
Md Ataur Rahman ◽  
Nusrat Ahmed ◽  
Ikramul Hasan ◽  
Md Selim Reza
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Product Yield ◽  
Drug Content ◽  
S 100 ◽  
Emulsification Solvent Evaporation ◽  
Eudragit S 100

In the present study naproxen loaded microspheres were prepared by emulsification solvent evaporation method in order to achieve targeted drug delivery. Eudragit L 100 and Eudragit S 100 were used as the rate retardant polymers in the preparations. Thirteen formulations (F1-F13) were prepared using 22 factorial design by changing the concentration of these two polymers. All the formulations were evaluated for product yield, drug content, entrapment efficiency, particle size and drug release profiles. Highest drug content and entrapment efficiency were found to be 30.17% (F4) and 91.86% (F8) respectively. The particle size was found to be 159.26-234.70 ?m for all formulations. In-vitro drug release studies were performed using USP type II (Paddle) apparatus for 8 hrs in pH 7.4 phosphate buffer. The maximum drug release after 8 hrs was found to be 60.19% for batch F4. The release kinetics of all formulations were evaluated by using zero order, first order, Higuchi, Korsmeyer-Peppas, Kopcha and Hixson Crowell model. Almost all formulations fitted best with the Kopcha kinetic model. The SEM study indicated the spherical structure of the microspheres having rough surfaces.Dhaka Univ. J. Pharm. Sci. 15(1): 47-55, 2016 (June)

scholarly journals Enhancement of Solubility and Dissolution Rate of Poorly Soluble Drug Nifedipine by Solid Sedds

2020 ◽  
Vol 10 (01) ◽  
pp. 9-15
Author(s):  
Sabitri Bindhani ◽  
Utkalika Mohapatra ◽  
Snehamayee Mohapatra ◽  
Rajat K. Kar
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Particle Size Analysis ◽  
Sem Analysis ◽  
In Vitro Dissolution ◽  
Size Analysis ◽  
Drug Content

Nifedipine is a dihydropyridine calci channel blocking agent belongs to biopharmaceutical classification system (BCS) class-II mainly applied in the treatment of hypertension and angina-pectoris. The objective of this work is to improve the solubility and dissolution rate of nifedipine by formulating into a solid-self micro emulsifying drug delivery system (solid smedds). Methods: Oil, Surfactant, and cosurfactant were selected by solubility screening study. For the determination of the best emulsion region, a pseudo ternary diagram was prepared. Based on solubility castor oil, tween 80 and polyethylene glycol (PEG) 400 was selected in which SCOSmix (a mixture of surfactant and cosurfactant) was 1:1. Thermodynamic stability study was performed for the determination of stable smedds formulation. These formulations were evaluated for self emulsification time, drug content analysis, robustness to dilution test, particle size analysis, and in vitro diffusion study. The optimized formulation was selected for formulating into solid-smedds by using aerosil 200 at a different ratio. SCF9L (0.65:1) was selected due to its good flow property. Then it was evaluated for particle size analysis, drug content study, differential scanning calorimetry (DSC), X-Ray Diffraction study (XRD), fourier transform infrared spectroscopy (FTIR) Scanning Electron Microscopy study (SEM) analysis, and in vitro dissolution study. Results: DSC and XRD result shows that the drug within the formulation was in the amorphous state. From the SEM analysis, the texture of powder showed a uniform granular structure, and there was no incompatibility between drugs. Excipients was observed from ftir study. From the in vitro dissolution study, it improved the dissolution rate of nifedipine, which was 98.68% of drug release, where pure drug release only 6.75%.

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