scholarly journals Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

2021 ◽  
Author(s):  
Shahjaman Halder ◽  
Sourav Poddar ◽  
Jasmina Khanam
Keyword(s):  
Drug Release ◽  
Scale Up ◽  
Control Release ◽  
Entrapment Efficiency ◽  
Ft Ir ◽  
Dermal Delivery ◽  
Size Of Particles ◽  
Average Size ◽  
Porous Morphology ◽  
Double Emulsification

Abstract The present investigation aims at developing models by response surface methodology (FCCCD) followed by the scale-up method in preparing control release microsponge particles loaded with 5- fluorouracil, a drug used to treat actinic keratosis and colon cancer, and producing a new Dermal Delivery System. The polymer-based (ethyl cellulose and eudragit RS 100) microsponge particles were prepared by the w/o/w double emulsification method. The optimized product was formed with the combination of independent variables levels: polymer (600 mg), stirring speed (1198 rpm) and surfactant (2% w/v), yielding responses as yield (~63.6257%), the average size of particles (~151.563 µm), entrapment efficiency (~75.319 %) and drug release in 8hr (~75.75%), with desirability value of 0.737. The products showed similar responses as obtained in scale-up work. FT-IR, DSC and SEM studies confirmed the drug's compatibility with polymers and porous morphology. Finally, gel embedded optimised product showed shear-thinning rheological property, ideal for drug release from the thixotropic gel.

Development of Biodegradable Injectable In situ Forming Implants for Sustained Release of Lornoxicam

2018 ◽  
Vol 16 (1) ◽  
pp. 66-78 ◽  
Author(s):  
Ruby Christian ◽  
Vaishali Thakkar ◽  
Tushar Patel ◽  
Mukesh Gohel ◽  
Lalji Baldaniya ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Maximum Plasma ◽  
Sustained Drug Release ◽  
Drug Entrapment Efficiency ◽  
Ft Ir

Objective: The focus of this study was to develop in situ injectable implants of Lornoxicam which could provide sustained drug release. Methods: Biodegradable in situ injectable implants were prepared by polymer precipitation method using polylactide-co-glycolide (PLGA). An optimized formulation was obtained on the basis of drug entrapment efficiency, gelling behavior and in vitro drug release. The compatibility of the formulation ingredients were tested by Fourier transform infrared (FT-IR) spectroscopy, and differential scanning colorimetry (DSC). SEM study was performed to characterize in vivo behavior of in situ implant. Pharmacokinetic study and in vivo gelling study of the optimized formulation were performed on Sprague-Dawley rats. Stability testing of optimized formulation was also performed. Results: The drug entrapment efficiency increased and burst release decreased with an increase in the polymer concentration. Sustained drug release was obtained up to five days. SEM photomicrographs indicated uniform gel formation. Chemical interaction between the components of the formulation was not observed by FT-IR and DSC study. Pharmacokinetic studies of the optimized formulation revealed that the maximum plasma concentration (Cmax), time to achieve Cmax (Tmax) and area under plasma concentration curve (AUC) were significantly higher than the marketed intramuscular injection of lornoxicam. Stability study of optimized batch showed no change in physical and chemical characteristics. Conclusion: Lornoxicam can be successfully formulated as in situ injectable implant that provides long-term management of inflammatory disorders with improved patient compliance.

FORMULATION AND STATISTICAL OPTIMIZATION OF MULTIPARTICULATE LAFUTIDINE-LOADED GASTRORETENTIVE DELIVERY SYSTEM USING 32- FACTORIAL DESIGN

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (10) ◽  
pp. 43-54
Author(s):  
K.A Sapate ◽  
◽  
P. V. Dangre ◽  
M. D. Godbole
Keyword(s):  
Drug Release ◽  
Interaction Analysis ◽  
Optimization Technique ◽  
Entrapment Efficiency ◽  
Gastric Fluid ◽  
Fed State ◽  
32 Factorial Design ◽  
Predicted Values ◽  
Average Size

The purpose of this research was to develop and optimize buoyant beads containing lafutidine by ionic-gelation method for gastroretentive delivery. The effect of two independent process variables like NaHCO 3: Polymer, Drug: Polymer ratio on % drug entrapment, % swelling and % drug release of buoyant beads containing lafutidine was optimized using 32 factorial designs. The observed responses coincided well with the predicted values, given by the optimization technique. The optimized beads showed drug entrapment efficiency 78.76+0.27%, swelling 69.90+0.13%, cumulative drug release 69.00+0.36% after 8 h; the average size of all buoyant beads ranged from 1.35+0.01 to 1.56+0.05 mm. The buoyant beads were characterized by SEM, DSC and FTIR spectroscopy for surface morphology and excipient-drug interaction analysis, respectively. All these beads showed prolong release of lafutidine over 8 h in 0.1 N HCl (pH1.2) evaluation of buoyancy of the optimized formulation in vivo in human volunteers showed that the beads were buoyant in gastric fluid for 8 h both in fasted and fed state.

scholarly journals Formulation & InVitro Evaluation of Controlled Release Tablets of Oxcarbazepine

2021 ◽  
pp. 58-68
Author(s):  
N.Phrudvish ◽  
T.Malyadri ◽  
Ch.Saibabu
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Release Kinetics ◽  
Control Release ◽  
In Vitro Dissolution ◽  
Compatibility Studies ◽  
Ft Ir ◽  
Controlled Release Tablets

The present research project aimed to develop a Control release oral Oxcarbazepine tablets by using Polymers like Tamarind gum, Xanthan gum, HPMC K4M, and HPMC K 15M were used for controlling the drug release, and the polymers are mixed in a predetermined ratio. Totally 12 formulations were prepared and evaluated for pre-compression and post-compression parameters, and all the results were found to be within the limits. From the drug and excipients compatibility studies(FT-IR) it was confirmed that the drug and excipients have any interactions. The in vitro dissolution studies revealed that the F12 formulation containing 18% of HPMC K4M & 18% of HPMC K15M controls the drug release up to 12hours. So F12 formulation was considered to be suitable for the formulation of Oxcarbazepine controlled-release tablets at 18% concentration of HPMC K4M & 18% concentration of HPMC K15M and the drug release kinetics revealed that the F12 formulation shows a super case II transport mechanism.

Acyclovir Loaded Solid Lipid Nanoparticle Based Cream: A Novel Drug Delivery System

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
EL- Assal I. A. ◽  
Retnowati .
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Antiviral Agent ◽  
Study Drug ◽  
Particle Size Analysis ◽  
Stability Study ◽  
Size Analysis ◽  
Solid Lipid ◽  
Dermal Delivery

Objective of the present investigation was enthused by the possibility to develop solid lipid nanoparticles (SLNs) of hydrophilic drug acyclovir. Also study vitro and vivo drug delivery. Methods: Drug loaded SLNs (ACV-SLNs) were prepared by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state with formula optimization study (Different lipid concentration, drug loaded, homogenization / stirring speed and compritol 888ATO: drug ratio). ACV - SLN incorporated in cream base. The pH was evaluated and rheological study. Drug release was evaluated and compared with simple cream- drug, ACV – SLN with compritol 888ATO and marketed cream. The potential of SLN as the carrier for dermal delivery was studied. Results: Particle size analysis of SLNs prove small, smooth, spherical shape particle ranged from 150 to 200 nm for unloaded and from 330 to 444 nm for ACV loaded particles. The EE% for optimal formula is 72% with suitable pH for skin application. Rheological behavior is shear thinning and thixotropic. Release study proved controlled drug release for SLNs especially in formula containing compritol88 ATO. Stability study emphasized an insignificant change in SLNs properties over 6 month. In-vivo study showed significantly higher accumulation of ACV in stratum corneum, dermal layer, and receptor compartment compared with blank skin. Conclusion: AVC-loaded SLNs might be beneficial in controlling drug release, stable and improving dermal delivery of antiviral agent(s).

Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Anamika Saxena Saxena ◽  
Santosh Kitawat ◽  
Kalpesh Gaur ◽  
Virendra Singh
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Entrapment Efficiency ◽  
Repeated Administration ◽  
Alginate Beads ◽  
Delivery Systems ◽  
Sem Analysis ◽  
Formulation Development

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.

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.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

2017 ◽  
Vol 23 (3) ◽  
pp. 467-480 ◽  
Author(s):  
Satyanarayan Pattnaik ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Molecular Sieves ◽  
Release Kinetics ◽  
Drug Loading ◽  
Scale Up ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Water Soluble Drugs ◽  
Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

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.

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