scholarly journals Formulation and Optimization of Sustained Release Stavudine Microspheres Using Response Surface Methodology

2011 ◽  
Vol 2011 ◽  
pp. 1-7 ◽  
Author(s):  
Sanjay Dey ◽  
Soumen Pramanik ◽  
Ananya Malgope
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
Independent Variables ◽  
Optimum Formulation ◽  
Dependent Variables ◽  
High Entrapment Efficiency ◽  
Full Factorial

The aim of the current study was to formulate and optimize the formulation on the basis of in vitro performance of microsphere. A full factorial design was employed to study the effect of independent variables, polymer-to-drug ratio () and stirring speed (), on dependent variables, encapsulation efficiency, particle size, and time to 80% drug release. The best batch exhibited a high entrapment efficiency of 70% and mean particle size 290 μm. The drug release was also sustained for more than 12 hours. The study helped in finding the optimum formulation with excellent sustained drug release.

scholarly journals Formulation and Invitro characterization of Flurbiprofen loaded Nanosponges

2021 ◽  
Vol 12 (3) ◽  
pp. 1798-1802
Author(s):  
Gangadhara R. ◽  
Satheesh K. P. ◽  
Devanna N. ◽  
Sasikala L. ◽  
Vandavasi Koteswara Rao
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Guar Gum ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Topical Gel ◽  
High Entrapment Efficiency

The aim of this analysis is to see how effective a Nanosponge-loaded topical gel is at distributing flurbiprofen through the skin. Flurbiprofen was entrapped in Nanosponge and formulated into a gel for this purpose. Flurbiprofen Nanosponges were developed by solvent evaporation using pluronic F68 and ethyl cellulose. The particle size and entrapment quality were discovered to be in the range of 200-410 nm and 90.94% to 98.68%, respectively. For gel formulation, Nanopsonges with high entrapment efficiency and the smallest particle size (F3) were chosen based on the characterization. Using Guar gum, Carbopol, and HPMC K4M, a total of 6 formulations were produced to determine the sustained drug release and were tested for physiochemical tests, producing positive results. According to the findings of the above in vitro drug release trials, formulations containing carbopol release more drug at the end of 11 hours than other formulations and follow a zero-order with case II transport mechanism.

scholarly journals Development and In-Vitro Evaluation of Budesonide Mucoadhesive Microspherefor Pulmonary Drug Delivery

2021 ◽  
Vol 11 (2-S) ◽  
pp. 76-81
Author(s):  
Jddtadmin Journal
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Chemical Interaction ◽  
Entrapment Efficiency ◽  
Pulmonary Drug Delivery ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency

Thepurpose of the study was to develop and evaluatemucoadhesive microspheres of Budesonide for pulmonary drug delivery systemhaving prolonged residence time and sustained drug release. Microspheres were prepared by emulsificationsolvent evaporation technique using HPMC, carbopol as polymers in varying ratios. The microspheres were evaluated for its percentage yield, drug entrapment efficiency, particle size and shape, in vitro mucoadhesion study and in vitro drug release studies.The FTIR studies revealed no chemical interaction between the drug molecule and polymers and found that drug was compatible with used polymer. The mucoadhesive microspheres showed particle size, drug entrapment efficiency and yield in the ranges of148 - 164 μm, 68.0 - 85.0%and67.52 - 87.25% respectively. In vitro drug release and mucoadhesion study confirms thatformulationF5 was the best formulation as it releases 81.8 % at the end of 12 hr. in controlled manner and percentage mucoadhesion of 75.2 % after 10 hr. This confirms the developed budesonidemucoadhesive microspheres are promising for pulmonary drug delivery system.   Keywords: Budesonide, Mucoadhesion, Microspheres, Drug entrapment efficiency.

scholarly journals Formulation And Evaluation Of Floating Microspheres Of Cefdinir

2021 ◽  
Vol 23 (11) ◽  
pp. 906-929
Author(s):  
Jeslin. D ◽  
◽  
Nithya Kalyani.K ◽  
Padmaja. V ◽  
Suresh Kumar.P ◽  
...  
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
Magnetic Systems ◽  
Gastric Residence Time ◽  
Gum Karaya ◽  
High Entrapment Efficiency ◽  
Full Factorial ◽  
Good Flow

Various approaches have been used to retain the dosage form in the stomach as a way ofincreasing the gastric residence time (GRT), including floatation systems; high-density systems; mucoadhesive systems; magnetic systems; unfoldable, extendible, or swellable systems; andsuperporous hydrogel systems. The aim of this study was to prepare and evaluate floatingmicrospheres of cefdinir for the prolongation of gastric residence time. Themicrospheres were prepared byCapillary Extrusion method.A full factorial design was applied to optimize the formulation. The optimum batch of microsphere exhibited smooth surfaces with good flow and packing properties, prolonged sustained drug release, remained buoyant for more than 12 hrs, high entrapment efficiency upto68%.Scanning electron microscopy confirmed the hollown structure with particle size in the order of190 μm. The studies revealed that increase in concentration of gum Karaya increased the drug release from the floating microspheres.

scholarly journals Preparation and Evaluation of Intraperitoneal Long-Acting Oxaliplatin-Loaded Multi-Vesicular Liposomal Depot for Colorectal Cancer Treatment

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 736
Author(s):  
Sharif Md Abuzar ◽  
Eun Jung Park ◽  
Yeji Seo ◽  
Juseung Lee ◽  
Seung Hyuk Baik ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Lag Phase ◽  
Burst Release ◽  
Sustained Drug Release ◽  
Long Acting ◽  
High Entrapment Efficiency

Colorectal cancer with peritoneal metastasis has a poor prognosis because of inadequate responses to systemic chemotherapy. Cytoreductive surgery followed by intraperitoneal (IP) chemotherapy using oxaliplatin has attracted attention; however, the short half-life of oxaliplatin and its rapid clearance from the peritoneal cavity limit its clinical application. Here, a multivesicular liposomal (MVL) depot of oxaliplatin was prepared for IP administration, with an expected prolonged effect. After optimization, a combination of phospholipids, cholesterol, and triolein was used based on its ability to produce MVL depots of monomodal size distribution (1–20 µm; span 1.99) with high entrapment efficiency (EE) (92.16% ± 2.17%). An initial burst release followed by a long lag phase of drug release was observed for the MVL depots system in vitro. An in vivo pharmacokinetic study mimicking the early postoperative IP chemotherapy regimen in rats showed significantly improved bioavailability, and the mean residence time of oxaliplatin after IP administration revealed that slow and continuous erosion of the MVL particles yielded a sustained drug release. Thus, oxaliplatin-loaded MVL depots presented in this study have potential for use in the treatment of colorectal cancer.

scholarly journals FORMULATION AND EVALUATION OF MOISTURIZING CREAM CONTAINING SUNFLOWER WAX

2018 ◽  
Vol 10 (11) ◽  
pp. 54 ◽  
Author(s):  
Avish D. Maru ◽  
Swaroop R. Lahoti
Keyword(s):  
Particle Size ◽  
Stearic Acid ◽  
Physicochemical Parameters ◽  
Research Work ◽  
Independent Variables ◽  
Dependent Variables ◽  
Full Factorial ◽  
32 Full Factorial Design ◽  
Sunflower Wax

Objective: The main objective of the present investigation was to design, prepare and evaluate moisturizing cream using sunflower wax.Methods: In the present work 32 full factorial design was applied to study the effect of varying concentration of independent variables stearic acid (X1) and sunflower wax (X2) on dependent variables viscosity and spreadability. All of the prepared formulations of moisturizing cream were evaluated for its physicochemical parameters. Further, the optimized formulation and selected commercial moisturizer compared and evaluated for its physicochemical parameters like pH, particle size, spreadability, viscosity and in vitro occlusivity test.Results: Nine different formulations of the moisturizing cream were prepared and all the findings obtained were within the prescribed limit. When compared to the prototype formulation of cream, the formulation MF5 showed good viscosity, in vitro occlusivity and spreadability. From the nine different formulations, MF5 containing 2 % stearic acid and 2 % sunflower was chosen as the optimized formula. Optimization was done on the basis of in vitro occlusivity studies and physicochemical parameters.Conclusion: The results obtained in this research work clearly showed a promising potential of moisturizing cream containing a specific ratio of stearic acid and sunflower wax as emulsifiers. Thus it can be concluded that sunflower wax is incorporated in the moisturizing cream, to avail of its cosmetic benefits.

scholarly journals Development and Characterization of Mitoxantrone-Loaded Glutaraldehyde Crosslinked Sodium Alginate Nanoparticles for the Delivery of Anticancer Drugs

2021 ◽  
pp. 18-24
Author(s):  
Muhammad Wahab Amjad ◽  
Maria Abdul Ghafoor Raja
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sodium Alginate ◽  
Anticancer Drugs ◽  
Antineoplastic Agent ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
Drug Entrapment Efficiency

Every year millions of new cases of various types of cancers are diagnosed, leading to an alarming rate of fatalities. Mitoxantrone is an anthracenedione antineoplastic agent which is used in the treatment of various types of cancer, mostly acute myeloid leukemia and prostate cancer. In spite of its therapeutic applications, it possesses numerous limitations and side effects including specific targeting and systemic toxicity. Sodium alginate is a biodegradable, mucoadhesive and biocompatible polymer commonly used in drug delivery applications. Glutaraldehyde is a saturated dialdehyde and is used as a polymer cross linker. In this study, mitoxantrone-loaded glutaraldehyde-sodium alginate nanoparticles were developed by ionic gelation method and characterized (determination of particle size, drug entrapment efficiency, drug release and its kinetics) for the delivery of anticancer drugs. The nanoparticles mean particle size was found to be within the acceptable range. The entrapment efficiency was also on the higher side with sustained drug release. The findings of this study reveal promising potential of delivery system and project the way forward for further in vitro and in vivo investigations.

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

Design and Evaluation of Long Acting Biodegradable PLGA Microspheres for Ocular Drug Delivery

2019 ◽  
Vol 10 ◽  
Author(s):  
Anjali Pandya ◽  
Rajani Athawale ◽  
Durga Puro ◽  
Geeta Bhagwat
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Degradation Products ◽  
Ex Vivo ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Rational Approach ◽  
Plga Microspheres ◽  
Long Acting

Background: The research work involves development of PLGA biodegradable microspheres loaded with dexamethasome for intraocular delivery. Objective: To design and evaluate long acting PLGA microspheres for ocular delivery of dexamethasone. Method: Present formulation involves the development of long acting dexamethasone loaded microspheres composed of a biodegradable controlled release polymer, Poly(D, L- lactide-co-glycolide) (PLGA), for the treatment of posterior segment eye disorders intravitreally. PLGA with monomer ratio of 50:50 of lactic acid to glycolic acid was used to achieve a drug release up to 45 days. Quality by Design approach was utilized for designing the experiments. Single emulsion solvent evaporation technique along with high pressure homogenization was used to facilitate formation of microspheres. Results: Particle size evaluation, drug content and drug entrapment efficiency were determined for the microspheres. Particle size and morphology was observed using Field Emission Gun-Scanning Electron Microscopy (FEG-SEM) and microspheres were in the size range of 1-5 μm. Assessment of drug release was done using in vitro studies and transretinal permeation was observed by ex vivo studies using goat retinal tissues. Conclusion: Considering the dire need for prolonged therapeutic effect in diseases of the posterior eye, an intravitreal long acting formulation was designed. Use of biodegradable polymer with biocompatible degradation products was a rational approach to achieve this aim. Outcome from present research shows that developed microspheres would provide a long acting drug profile and reduce the frequency of administration thereby improving patient compliance.

scholarly journals FORMULATION, OPTIMIZATION AND IN VITRO EVALUATION OF 5-FLUOROURACIL LOADED LIQUORICE CRUDE PROTEIN NANOPARTICLES FOR SUSTAINED DRUG DELIVERY USING BOX-BEHNKEN DESIGN

2021 ◽  
pp. 216-226
Author(s):  
GEETHA V. S. ◽  
MALARKODI VELRAJ
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Crude Protein ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Sustained Drug Delivery ◽  
Drug Loading Efficiency

Objective: To formulate, optimize and evaluate 5-fluorouracil loaded liquorice crude protein nanoparticles for sustained drug delivery using Box-Behnken design. Methods: 5-fluorouracil (5-FU) loaded liquorice crude protein (LCP) nanoparticles were prepared by desolvation method using ethanol-water (1:2 ratio), Tween-80 (2%v/v) as stabilizing agent and gluteraldehyde (8% v/v) as cross linking agent. The optimization of prepared nanoparticles was carried out using Box-Behnken design with 3 factors 2 levels and 3 responses. The independent variables were A)5-FU concentration B)LCP concentration and C) sonication time while the responses were R1) Drug entrapment efficiency R2) Drug loading efficiency and R3) Particle size. The correlation between factors and responses were studied through response surface plots and mathematical equations. The nanoparticles were evaluated for FTIR, physicochemical properties like particle size and zeta potential by Photon correlation spectroscopy (PCS) and surface morphology by TEM. The entrapment efficiency, drug loading efficiency and in vitro drug release studies in PBS pH 7.4 (24 h) were carried out. The observed values were found to be in close agreement with the predicted value obtained from the optimization process. Results: 5-fluorouracil loaded LCP nanoparticles were prepared by desolvation method, the optimization was carried out by Box-Behnken design and the final formulation was evaluated for particle size (301.1 nm), zeta-potential (-25.8mV), PDI(0.226), with entrapment efficiency (64.07%), drug loading efficiency (28.54%), in vitro drug release (65.2% in 24 h) respectively. The formulated nanoparticles show Higuchi model drug release kinetics with sustained drug delivery for 24 h in pH7.4 buffer. Conclusion: The results were proved to be the most valuable for the sustained delivery of 5-Fluorouracil using liquorice crude protein as carrier. 5-FU–LCP nanoparticles were prepared using Tween-80 as stabilizing agent and gluteraldehyde as cross-linking agent to possess ideal sustained drug release characteristics.

Preparation, Characterization and Optimization of Irbesartan Loaded Solid Lipid Nanoparticles for Oral Delivery

2021 ◽  
pp. 97-104
Author(s):  
Kumara Swamy S ◽  
Ramesh Alli
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Sustained Drug Release ◽  
Bioavailability Enhancement ◽  
Solid Lipid

The purpose of this study was to develop and evaluate irbesartan (IS) loaded solid lipid nanoparticles (SLNs; IS-SLNs) that might enhance the oral bioavailability of IS. IS, an angiotensin-receptor antagonist, used to treat hypertension. However, poor aqueous solubility and poor oral bioavailability has limited therapeutic applications of IS. Components of the SLNs include either of trimyristin/tripalmitin/tristearin/trilaurate/stearic acid/beeswax, and surfactants (Poloxamer 188 and soylecithin). The IS-SLNs were prepared by hot homogenization followed by ultrasonication method and evaluated for particle size, poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro drug release. The physical stability of optimized formulation was studied at refrigerated and room temperature for two months. The optimized IS-SLN formulation (F4) had a mean diameter of about 217.6±3.62 nm, PDI of 0.163±0.032, ZP of -28.5±4.12, assay of 99.8±0.51 and EE of 93.68±2.47%. The formulation showed sustained drug release compared with control formulation over 24 h. Optimized formulation was found to be stable over two months. IS-SLN showed nearly spherical in shape using and converted to amorphous form by DSC. Thus, the results conclusively demonstrated SLNs could be considered as an alternative delivery system for the oral bioavailability enhancement of IS.

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