scholarly journals Design and Characterization of Mucoadhesive Microspheres of Etodolac

2019 ◽  
Vol 11 (03) ◽  
Author(s):  
A R Shabaraya ◽  
A S Parulkar ◽  
D Shripathy ◽  
P Shetty
Keyword(s):  
Drug Targeting ◽  
Entrapment Efficiency ◽  
Specific Region ◽  
Zero Order ◽  
Solvent Evaporation Method ◽  
In Vitro Drug Release ◽  
Zero Order Kinetics ◽  
Central Composite

Mucoadhesive microspheres are drug delivery system intended for drug targeting to a specific region. Etodolac is a Non-steroidal anti-inflammatory drug. Sustain released Etodolac loaded mucoadhesive microspheres were prepared to overcome the relatively short residence time of Etodolac in the GIT tract before elimination. Solvent evaporation method was used for preparation of mucoadhesive microspheres with the help of Carbopol 974P, HPMC K100M and HPMC K4M as the polymers. Central composite design was selected for the development of the formulation. The formulations were evaluated for their particle size, surface morphology, degree of swelling, entrapment efficiency, drug content and in-vitro drug release study was done. Based on the results obtained from the preliminary formulations three optimized formulations were designed. The percentage mucoadhesion and swelling index of these formulations were obtained in the range of 66-70% and 82.50-83.84% respectively. Optimized formulation releases 90.94% to 92.11% of drug after 10 hours and follows zero order kinetics.

Design, development and characterization of ketorolac tromethamine polymeric nanosuspension

2019 ◽  
Vol 10 (9) ◽  
pp. 585-597 ◽  
Author(s):  
Pankaj A Jadhav ◽  
Adhikrao V Yadav
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Slight Reduction ◽  
Ketorolac Tromethamine ◽  
Design Development ◽  
In Vitro Drug Release ◽  
Sustained Effect ◽  
Eudragit Rl

Aim: At present, various ophthalmic formulations show low bioavailability. The rationale of present work was to design and develop stable ketorolac tromethamine nanosuspension with sustained effect and greater permeability for ocular drug delivery and increased ocular residence. Materials & methods: Formulations were designed by using central composite design, developed by combined nanoprecipitation and probe sonication method. Results & discussion: Nanosuspensions depicted the size range of the particles in between 199 and 441 nm with slight reduction in crystallinity of drug. In vitro drug release revealed that higher % entrapment efficiency of drug in nanosuspension delays the drug release. Conclusion: Eudragit RL-100-based nanosuspension increases viscosity and avoids problems like drug loss from precorneal surface and rapid drainage through nasolacrimal areas.

Formulation and evaluation of Cassia tora phytosomal gel using central composite design.

2021 ◽  
Vol 14 ◽  
Author(s):  
Leander Corrie ◽  
Raghunandan Gundaram ◽  
Latha Kukatil
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Therapeutic Activity ◽  
In Vitro Drug Release ◽  
Cassia Tora ◽  
Dependent Variables ◽  
Antifungal Effects ◽  
Two Parameters ◽  
Central Composite

Background:: Cassia tora has been classified as an antifungal agent, but no optimized formulation for improved drug penetration has been developed. Objective:: The present work aimed to formulate Cassia tora extract (CTE) phytosomal gel that could be used for its antifungal effects and improved therapeutic activity. Materials and Methods: The CTE phytosomes were formulated by varying the concentration of lecithin (0.15-0.25% w/v) and speed of rotation (100-160 rpm). A 22 factorial design was applied by taking the above two parameters as independent variables and vesicular size and entrapment efficiency as dependent variables. The phytosomes were also evaluated for polydispersity index, zeta potential and in vitro drug release. The optimized phytosomes of CTE were further developed into a gel, the optimized gel was also evaluated and stability studies were conducted. Results and Discussion: The optimized CTE phytosome showed a vesicular size of ~ 124 nm and entrapment efficiency of 95%. The CTE phytosomes showed a drug release of 58.79% in 24 hours following Higuchi's order of release. The CTE phytosomes were formulated into a gel by using 1% Carbopol 934 and were evaluated for pH, viscosity and homogeneity. The formulated gel showed better penetration than conventional gel and stability changes indicated no major changes to the CTE phytosomal gel. Conclusion: The optimized gel had better penetration and drug release than the conventional gel. Its therapeutic activity, therefore can be estimated to be enhanced.

scholarly journals Formulation and in vitro Evaluation of Piroxicam Emulgel

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
Y Bindu Vani ◽  
C. Surya Prakash Reddy
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Evaluation Studies ◽  
Tween 80 ◽  
Zero Order ◽  
In Vitro Drug Release ◽  
Zero Order Kinetics ◽  
Release Studies ◽  
Span 80

The present work is concerned with the formulation and evaluation of Piroxicam emulgel employing carbopol 934 and xanthan gum as polymers. The emulgel is prepared by combining the gel and emulsion. The gel in formulations were prepared by dispersing Carbopol 934 and xanthan gum separately in purified water with constant stirring at a moderate speed and then the pH was adjusted to 4 to 5.4 using Tri-ethanol amine (TEA). The oil phase in the emulsion consists of oleic acid and span-80. The aqueous phase in the emulsion was prepared using Tween-80, propylene glycol and distilled water. The prepared emulgel formulations were subjected to evaluation studies like Physical appearance, rheological studies, estimation of drug content and in-vitro drug release. The appearance of prepared emulgel was white. The pH of the emulgel was found to be 5.4. The in vitro drug release studies revealed that formulation F1 showed 85.20% and formulation F2 showed 79.23% of drug release at the end of 8 hrs. The drug release of F1 formulation follows zero order kinetics.

Formulation, optimization, and characterization of amlodipine besylate loaded polymeric nanoparticles

2021 ◽  
Vol 29 (9_suppl) ◽  
pp. S1555-S1568
Author(s):  
Vibha Chourasiya ◽  
Sarvesh Bohrey ◽  
Archna Pandey
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Polymeric Nanoparticles ◽  
Entrapment Efficiency ◽  
Amlodipine Besylate ◽  
Process Yield ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency

The objectives of this work were to formulate and optimize amlodipine besylate loaded polymeric nanoparticles by using factorial design. The emulsion solvent evaporation method was employed successfully to produce the drug loaded polymeric nanoparticles and the optimization was done by the help of the 24 factorial design. The effect of the main preparation variables on the dependent variables such as nanoparticle size and % drug entrapment efficiency was studied for the optimization of the nanoparticles. The characterization of these nanoparticles was done by the different parameters such as interaction between the excipients, size, morphology, zeta potential, % drug entrapment efficiency, % process yield, and in-vitro drug release behavior. FTIR, DLS, TEM, AFM, zeta potential studies, and dialysis bag method were performed for this purpose. The in vitro drug release data were analyzed by different kinetic models to know the release mechanism. The optimized nanoparticles were spherical in shape and showed particle size 91.5 ± 4.3 nm, PDI 0.368 ± 0.014, zeta potential −17.5 mV, % drug entrapment efficiency 74.06 ± 2.1%, and % process yield 78.51 ± 1.8%. The release kinetics studies revealed that drug release from the nanoparticles follow the Korsmeyer–Peppas model.

scholarly journals FORMULATION AND CHARACTERIZATION OF FLOATING BEADS OF ANTIBIOTIC BY EMULSION GELATION TECHNIQUE

2019 ◽  
pp. 57-62
Author(s):  
KHALIFA MY ◽  
SHAIKH SIRAJ N
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Microscopy Study ◽  
Generation Cephalosporin ◽  
Electron Microscopy Study ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Hydrogel Beads

Objective: The study aims at formulation and characterization of floating hydrogel beads of cefdinir for improving its bioavailability. Methods: Cefdinir is broad-spectrum, oral, third-generation cephalosporin antimicrobial agent active against Gram-positive and Gram-negative bacteria. The floating hydrogel beads of cefdinir were formulated with polymers such as sodium alginate and sodium carboxymethyl cellulose by emulsion gelation technique using olive oil/castor oil. The beads were evaluated for surface morphology, bead size, entrapment efficiency, floating characteristics, in vitro swelling, in vitro drug release, and stability studies. Results: On the basis of evaluation, all the beads show good swelling up to 12 h in 0.1 N hydrochloric acid. The swelling was followed by values in order of vegetable oil > mineral oil in case of emulsion gelation method. Scanning electron microscopy study shows that beads were spherical in shape. Comparing all the formulations, formulation FB12 was considered as optimized formulation which shows % yield 94.06±0.11, % floating 87.28±0.90, in vitro drug release 94.68, and also stable in stability studies. Conclusion: From the findings, it may be concluded that cefdinir-loaded floating beads were successfully prepared and proved to be useful for the better bioavailability and patient compliance for enhanced antimicrobial activity.

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 Characterization of Nanoemulsion Prepared from Self-emulsifying Rifampicin and its Antibacterial Effect on Staphylococcus aureus and Stap. epidermidis Isolated from Acne

2016 ◽  
Vol 14 (2) ◽  
pp. 171-177 ◽  
Author(s):  
Kohinur Begum ◽  
Amit Sarker ◽  
Israt Jahan Shimu ◽  
Md Mazharul Islam Chowdhury ◽  
Reza Ul Jalil
Keyword(s):  
Antibacterial Effect ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Stability Study ◽  
Ph Stability ◽  
Particle Sizes ◽  
In Vitro Drug Release ◽  
Drug Content

In this study, three different self emulsifying drug delivery systems of rifampicin (SEDD-R) were made using oleic acid and different surfactants such as Tween 80, Chremophor RH 40 and Chremophor EL designated as RN-TW, RN-CRH and RN- CEL. These self-emulsifying systems were converted to rifampicin nanoemulsion by adding water under sonication. The resulting particle sizes were found to be 192.7 nm, 183.4 nm and 179.2 nm for RN- CEL, RN-CRH and RN-TW, respectively using Zetasizer. Drug content, entrapment efficiency, in vitro drug release and pH stability tests was performed. Drug content and entrapment efficiency for RNTW, RN-CRH and RN- CEL were found as 0.9945% & 0.9835%, 0.9720% & 84.31% and 74.58 % & 56.89%, respectively. The release of drug from RN-TW, RN-CRH and RN-CEL occurred for 450-, 330- and 240- minutes, respectively. The pH stability study demonstrated that all formulations retained maximum drug at pH 5.8. Antibacterial effect of the preparations was evaluated against S. epidermidis and S. aureus isolated from acne and showed effective results.Dhaka Univ. J. Pharm. Sci. 14(2): 171-177, 2015 (December)

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

Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

2020 ◽  
Vol 10 (5) ◽  
pp. 649-663
Author(s):  
Reena Siwach ◽  
Parijat Pandey ◽  
Harish Dureja
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Class Ii ◽  
Dissolution Enhancement ◽  
In Vitro Drug Release ◽  
Bcs Class Ii

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability. Objective: : In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride. Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield. Result: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics. Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

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