scholarly journals Curcumin phytosomal softgel formulation: Development, optimization and physicochemical characterization

2015 ◽  
Vol 65 (3) ◽  
pp. 285-297 ◽  
Author(s):  
Ahmed N. Allam ◽  
Ibrahim A. Komeil ◽  
Ossama Y. Abdallah
Keyword(s):  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Formulation Development ◽  
Tem Analysis ◽  
Peg 400 ◽  
Naturally Occurring ◽  
Presystemic Metabolism ◽  
Flowing Powder ◽  
Lipophilic Molecule

Abstract Curcumin, a naturally occurring lipophilic molecule can exert multiple and diverse bioactivities. However, its limited aqueous solubility and extensive presystemic metabolism restrict its bioavailability. Curcumin phytosomes were prepared by a simple solvent evaporation method where free flowing powder was obtained in addition to a newly developed semisolid formulation to increase curcumin content in softgels. Phytosomal powder was characterized in terms of drug content and zeta potential. Thirteen different softgel formulations were developed using oils such as Miglyol 812, castor oil and oleic acid, a hydrophilic vehicle such as PEG 400 and bioactive surfactants such as Cremophor EL and KLS P 124. Selected formulations were characterized in terms of curcumin in vitro dissolution. TEM analysis revealed good stability and a spherical, self-closed structure of curcumin phytosomes in complex formulations. Stability studies of chosen formulations prepared using the hydrophilic vehicle revealed a stable curcumin dissolution pattern. In contrast, a dramatic decrease in curcumin dissolution was observed in case of phytosomes formulated in oily vehicles.

Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

1970 ◽  
Vol 1 (4) ◽  
pp. 349-356
Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate

Formulation development of matrix type transdermal patches containing mefenamic acid: physicochemical characterization and in vitro release evaluation

2017 ◽  
Vol 148 (7) ◽  
pp. 1215-1222 ◽  
Author(s):  
Jirapornchai Suksaeree ◽  
Kotchakorn Piamsap ◽  
Supawan Paktham ◽  
Tichakorn Kenprom ◽  
Chaowalit Monton ◽  
...  
Keyword(s):  
Mefenamic Acid ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Formulation Development ◽  
Matrix Type ◽  
Transdermal Patches ◽  
Vitro Release

scholarly journals FORMULATION DEVELOPMENT OF ORAL FAST-DISSOLVING FILMS OF RUPATADINE FUMARATE

2020 ◽  
pp. 67-72
Author(s):  
ABHIBRATA ROY ◽  
REEGAN AREES ◽  
MADHAVI BLR
Keyword(s):  
Drug Release ◽  
Inclusion Complex ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Solvent Casting ◽  
Formulation Development ◽  
Casting Method ◽  
Disintegration Time ◽  
Low Viscosity

Objective: Rupatadine fumarate (RF) is an anti-allergic drug indicated for the treatment of allergic rhinitis. It has low oral bioavailability due to its poor aqueous solubility and extensive hepatic first pass metabolism. In the present work, oral fast-dissolving films (OFDF) have been formulated and evaluated to facilitate dissolution in the oral cavity itself. Methods: Pullulan and HPMC (5, 15 cps) were employed as film formers and six formulations were tried. The physicochemical compatibility between drug and the polymers was studied by FTIR spectroscopy. RF-beta-cyclodextrin (BCD) inclusion complex was initially prepared and evaluated. The inclusion complex was incorporated into the film. OFDF were formulated and prepared by solvent casting method. The film size for one dose was 2 × 2 cm. The films were evaluated for various film parameters including disintegration time and drug release. Results: Preliminary film studies indicated % of film former solution to be between 3 and 5% for good appearance, mechanical strength, and quick disintegration. Solubility enhancement of RF is almost 40-fold from its BCD inclusion complex. Drug content in the films ranged between 83 and 90%. The pH ranged between 6 and 7 for all the formulations. All OFDF of RF disintegrated within one minute. With higher viscosity grade of HPMC, disintegration was comparatively slower and so was the drug release. Pullulan based films also showed desirable properties. F3 had disintegration time was 28 s and % drug release was 92% in 180 s. Conclusion: OFDF of RF could be formulated employing pullulan and HPMC low viscosity grades by solvent casting method. F3 containing HPMC E5 at 37% by weight of dry film showed desirable film properties. Stability studies indicated that there was no significant change in the films with respect to physicochemical properties and in vitro release.

scholarly journals Formulation Development and Evaluation of Liposphere of Poor Water Soluble Drug for Hyperlipidemia

2021 ◽  
Vol 11 (2) ◽  
pp. 23-30
Author(s):  
Anil Kumar ◽  
Umesh K. Jain ◽  
Ajay Patel
Keyword(s):  
Drug Release ◽  
Stearic Acid ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Water Soluble ◽  
Fibric Acid Derivative ◽  
Formulation Development ◽  
Bcs Class Ii ◽  
Paraffin Oil

Lipospheres offer a new approach to improve an aqueous solubility of BCS class-II drugs. Simvastatin is a third generation fibric acid derivative belonging to this class, employed clinically as a hypolipidemic agent to lessen the risk caused by atherosclerosis. An attempt was made to improve aqueous solubility of Simvastatin by aid of stearic acid and Paraffin oil. The factorial batches of the Simvastatin lipospheres were formulated by melt dispersion technique using 32 factorial design with variables X1- concentration of stearic acid and X2- concentration of paraffin oil and responses Y1 - % Drug Entrapment (% DE) and Y2 - % Drug Release (% DR). From the surface response graphs the optimized batch was formulated and evaluated for saturation solubility, in-vitro drug release studies. Significant improvement in the aqueous solubility of the drug in the Simvastatin lipospheres supports the applicability of lipospheres as a tool for improving aqueous solubility of the BCS class-II drugs. Keywords: Linospheres; Simvastatin; Drug release; Hyperlipidemic; Drug entrapment.

scholarly journals Microemulgel of Voriconazole: an Unfathomable Protection to Counter Fungal Contagiousness

Folia Medica ◽  
2017 ◽  
Vol 59 (4) ◽  
pp. 461-471 ◽  
Author(s):  
Kalpesh C. Ashara ◽  
Jalpa S. Paun ◽  
Moinuddin M. Soniwala ◽  
Jayant R. Chavda
Keyword(s):  
Water Solubility ◽  
In Vitro Study ◽  
Topical Delivery ◽  
Gelling Agent ◽  
Formulation Development ◽  
Solubility Study ◽  
Lattice Design ◽  
Peg 400 ◽  
Emulsification Property

AbstractBackground: Fluconazole and ketoconazole both have poor minimum inhibitory concentration than voriconazole. Voriconazole had serious side effects in oral and intravenous doses. It has poor water solubility. The objective of the study was to prepare and optimize microemulgel of voriconazole for topical delivery. Aim: Formulation, development, and evaluation of voriconazole microemulgel for topical delivery. Methods: Oil and emulsifi ers selected were on the basis of equilibrium solubility study and emulsification property respectively. The pseudo-ternary plot and constrained simplex lattice design were applied for preparation of microemulsions. Microemulsions were subjected to micelle size, zeta potential, polydispersity index, and in vitro study. They were optimized by Design-Expert®9.0.3.1 software. Formulation, development, evaluation and optimization of microemulgel were carried out. Microbial assay of an optimized batch of microemulgel was performed. Results: Solubility of voriconazole in Parker Neem®oil was 7.51±0.14 mg/g. Acrysol™K-150: PEG-400 in 4:1 ratio had the highest area for microemulsion. 59.2% Acrysol™K-150, 14.8% PEG-400, 11% Parker Neem®oil, 15% rose water, and 1% voriconazole as an optimized batch of microemulsion was selected for preparation of microemulgel. Carbomer 934P found a good gelling agent in 0-2% w/w concentration. An optimized batch of microemulgel had 0.974 desirability value. An optimized batch of microemulgel and Nizral®cream had 37.32±0.63% and 26.45±0.63% zones of inhibition. Conclusion: Topical antifungal treatment was successfully achieved with voriconazole microemulgel.

scholarly journals Physicochemical characterization and in vitro dissolution behaviour of celecoxib-β-cyclodextrin inclusion complexes

2007 ◽  
Vol 57 (1) ◽  
pp. 47-60 ◽  
Author(s):  
Vivek Sinha ◽  
R. Anitha ◽  
Soma Ghosh ◽  
Rachana Kumria ◽  
Jayant Bhinge ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Cyclodextrin Inclusion Complexes ◽  
Cyclodextrin Inclusion ◽  
Dissolution Behaviour ◽  
Poorly Soluble

Physicochemical characterization and in vitro dissolution behaviour of celecoxib-β-cyclodextrin inclusion complexes In this study, attempts were made to investigate the effects of β-cyclodextrin (β-CD) on the aqueous solubility and dissolution rate of celecoxib. Inclusion complexes were prepared by the kneading method and characterized by SEM, NMR, IR, DSC, and X-ray powder diffraction. Dissolution rate of the complexes was significantly greater than that of the corresponding physical mixtures and pure drug, indicating that the formation of inclusion complex increased the solubility of the poorly soluble drug celecoxib.

scholarly journals “FORMULATION DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING FILMS OF LAFUTIDINE”

2019 ◽  
Vol 7 (2) ◽  
Author(s):  
Hir. R. Mehta ◽  
Vijay K. Patel
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Stability Study ◽  
Formulation Development ◽  
Casting Technique ◽  
Drug Content ◽  
Peg 400 ◽  
Weight Variation ◽  
Folding Endurance

The present invention was aimed to formulate and evaluate Lafutidine gastro retentive films. The films were prepared by solvent casting technique using different film forming polymers like HPMC and Ethyl cellulose. PEG 400 used as a plastsizer. The prepared films were evaluated for number of parameters like Physical appearance, Weight variation, Thickness, Folding endurance, Tensile strength, unfolding behavior, floating properties, drug content and In vitro drug release studies. From the trial batches the best release for gastroretentive film was shown by formulation T5 (Ethyl cellulose and PEG 400). Formulation T5 exhibited good appearance, better mechanical strength with acceptable flexibility. Also, formulation T5 was given more than 90 % drug released after 12 hr and 97.56 % Drug content.  For optimization of formulation, 32 factorial design was applied by taking Ethyl cellulose and PEG 400 as an independent variables. Drug release at 8 hour and folding endurance selected as dependent variables. Based on drug release study, L8 batch found most satisfactory in all formulation and the effect of Ethyl cellulose and PEG 400 found significant. L8 batch found stable during stability study. Key words: Lafutidine, Floating Films, Ethyl Cellulose.

scholarly journals Formulation, Development, and Optimization of Anti- Hypertensive Nisoldipine Extended-Release Tablet Formulation

2020 ◽  
Vol 5 (03) ◽  
pp. 37-44
Author(s):  
Kukkadapu Pavan Kumar ◽  
Katta Sunand ◽  
Nerella Mounika ◽  
Mohammed Abdul Samad ◽  
A. Madhu Babu ◽  
...  
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Aqueous Solubility ◽  
Cellular Membrane ◽  
Tablet Formulation ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Formulation Development ◽  
Release Tablet

A drug molecule has to be water-soluble to be readily delivered to the cellular membrane. Many drugs are waterinsoluble, which creates numerous problems in the development of dosage forms. Controlled drug delivery formulation releases the drug with controlled kinetics for days and months, reducing the frequency of dosing, minimizing side effects, and improving patient compliance. Nisoldipine is a calcium channel antagonist that is indicated for the treatment of hypertension with very poor aqueous solubility. Thus, there is a need to improve the rate of drug release. Hence, the study was carried out to design, formulate and evaluate sustained-release tablet formulation of nisoldipine. Nisoldipine controlled release matrix tablets were prepared by roll compaction method. Preformulation studies have confirmed the purity and compatibility of drug with excipients used in the formulation. Pre-compression studies have confirmed the stability of formulation blends for compression. All the prepared formulations were evaluated for various physical and compression parameters such as bulk and tapped density, hardness, friability, and in vitro drug release studies. The results of drug release from prepared compressed nisoldipine extended-release tablets were found to be within the desired range.

scholarly journals Indocyanine Green Loaded Polymeric Nanoparticles: Physicochemical Characterization and Interaction Studies with Caco-2 Cell Line by Light and Transmission Electron Microscopy

Nanomaterials ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 133 ◽  
Author(s):  
Antonella Obinu ◽  
Elisabetta Gavini ◽  
Giovanna Rassu ◽  
Federica Riva ◽  
Alberto Calligaro ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Transmission Electron Microscopy ◽  
Indocyanine Green ◽  
Antitumor Agents ◽  
Polymeric Nanoparticles ◽  
Physicochemical Characterization ◽  
Tem Analysis ◽  
Transmission Electron

Biomedical applications of nanoparticles (NPs) have reached an increasing development in recent years. Recently, we demonstrated that newly synthesized poly (ethyl 2-cyanoacrylate) nanoparticles (PECA-NPs) are possible antitumor agents due to their cytotoxicity for cancer cells. Indocyanine green (ICG), an amphiphilic tricarbocyanine fluorescent dye, is widely used for the detection of tumoral extension in different organs during clinical surgery. Moreover, this fluorescent agent is unstable and it has a rapid clearance in physiological conditions in vivo. In this study, ICG was charged in PECA-NPs to improve its aqueous stability and make easier its use for the identification of tumor cells. Microscopic and ultrastructural aspects concerning the related in vitro interactions between ICG-loaded NPs and tumor cell culture were investigated. Obtained results showed an effective stabilization of ICG; furthermore, color inclusions inside the cells treated with ICG-loaded NPs demonstrated the internalization of NPs with associated ICG. Transmission electron microscopy (TEM) analysis demonstrated the cytoplasmic presence of coated vesicles (Ø ≤ 100 nm), hypothesizing their involvement in the mechanism of endocytosis. Therefore, ICG-loaded NPs could be proposed as agents for tumor diagnosis, hypothesizing also in the future a specific therapeutic treatment.

scholarly journals Development of nanostructured lipid carriers containing the antimicrobial ciprofloxacin for topical application

2019 ◽  
Author(s):  
Talita Cesarim Mendonça ◽  
Eneida de Paula ◽  
Simone R. Castro ◽  
Marcelo Lancellotti ◽  
Lígia N. M. Ribeiro
Keyword(s):  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Nanostructured Lipid Carriers ◽  
Zeta Potentials ◽  
Technological Potential ◽  
Antibiotic Effect ◽  
Antimicrobial Susceptibility Tests ◽  
Pharmaceutical Form ◽  
Susceptibility Tests

Ciprofloxacin (CIP), a broad spectrum antibacterial agent from the fluoroquinolone family, blocks the activity of the bacterial DNA gyrase. CIP has a limited aqueous solubility and fast clearance rate. Nanostructured lipid carriers (NLC) are drug delivery carriers very appropriate to upload hydrophobic drugs, improving their bioavailability, stability and potency. This work describes the development of NLC containing CIP, their physicochemical characterization and antimicrobial activity, in vitro. NLC particles (215-355 nm) of low size polidispersion (PDI 0.08-0.31) and negative zeta potentials (|20.7-38.7| mV) were prepared; scanning electron microscopy revealed their spherical shapes and regular contour. The particles remained stable during 365 days of storage at 25°C. The encapsulation efficiency of CIP ranged from 72.5 - 95.2%, with a sustained release profile (48 h). Preliminary antimicrobial susceptibility tests revealed a 30% increase in CIP action, when encapsulated in NLC. These proof-of-concept results show the great pharmaceutical and technological potential of the developed nanoformulations. After further tests we believe that NLC-CIP can come to be a novel pharmaceutical form to potentiate the antibiotic effect, reducing its dosage and undesirable side effects.

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