scholarly journals Development of Licorice Flavonoids Loaded Microemulsion for Transdermal Delivery Using CCD-Optimal Experimental Approach: Formulation Development and Characterization

2021 ◽  
Vol 3 ◽  
Author(s):  
Yang Xin ◽  
Shi Yun ◽  
Lu Yuhe ◽  
Mao Yinxue ◽  
Niu Shurui ◽  
...  
Keyword(s):  
Droplet Size ◽  
High Performance ◽  
Ternary Phase Diagram ◽  
Entrapment Efficiency ◽  
Skin Layer ◽  
Isopropyl Myristate ◽  
Formulation Development ◽  
Drug Content ◽  
Light Yellow ◽  
Light Yellow Color

In this research, we sought to surmount the poor dissolvability and transdermal absorption rate of licorice flavonoids (LFs) by fabricating a LFs microemulsion. LFs content was determined using high performance liquid chromatography. Initial studies such as dissolution testing, emulsification testing, and pseudo ternary phase diagram generation were implemented for screening components and optimized adopting the central composite design. While the tested responses were solubility, droplet size and PDI, thirteen trials were performed using two different variables, oil percentage and optimized emulsifier and co-emulsifier ratio. Microemulsions were then characterized for droplet size, PDI, transmission electron microscopy, viscosity, electrical conductivity, pH, entrapment efficiency, drug content and stability. Additionally, skin release profile, percutaneous absorption and retention were investigated adopting Franz diffusion cell. The optimal formulation was found to compose of laureth-9 (emulsifier, 6.72 g), propylene glycol (co-emulsifier, 1.80 g), isopropyl myristate (IPM, oil, 1.48 g), LFs (1.50 g) and at least more than 85% deionized water. The optimized and storage for 3 months of microemulsion was found to clear, light yellow color without phase separation or precipitation indicated the stability of the preparation to long-term placement. The mean droplet size, PDI, entrapment efficiency and drug content were discovered as 12.68 ± 0.12 nm, 0.049 ± 0.005, 97.28 ± 0.13% and 122.67 ± 0.40 mg·g−1, respectively. Furthermore, the optimal formulation sustained release LFs, remarkably deliver more LFs through the skin layer (644.95 ± 6.73 μg cm−2) and significantly retained LFs in the skin layer (9.98 μg cm−2). The study concluded that optimized microemulsion has potential and enhanced the dissolvability and cumulative penetration amount of LFs.

scholarly journals MSc. Development of the In-house Specifications and Study of the Stability of Self-nanoemulsifying Drug Delivery System Containing Rosuvastatin

2020 ◽  
Vol 36 (4) ◽  
Author(s):  
Phan Thi Nghia ◽  
Tran Thi Hai Yen ◽  
Vu Thi Thu Giang
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Droplet Size ◽  
Delivery System ◽  
Clinical Medicine ◽  
Entrapment Efficiency ◽  
Clinical Effectiveness ◽  
Stability Study ◽  
Formulation Development ◽  
The Stability

This study develops the in-house specifications of self-nanoemulsifying drug delivery system (SNEDDS) containing rosuvastatin based on the following criteria: description, identification, droplet size (≤200 nm) and polydiversity index (not more than 0.3), drug proportion in the oil phase (≥ 90.0%), assay (≥ 95.0% and ≤105.0% of the labeled amount of rosuvastatin (C22H28FN3O6S). The criteria were validated and the results were suitable for identification and determination of rosuvastatin in SNEDDS. Additionally, the results of the stability study show that the rosuvastatin SNEDDS met the criteria of description, droplet size, PDI, assay and drug rate in the oil phase for 12-month storage under the long-term condition (12 months) and 6 months on accelerated condition. Keywords Rosuvastatin, SNEDDS, specification, droplet size, entrapment efficiency. References [1] A. Luvai, W. Mbagaya, A.S. Hall, I.H. Barth, Rosuvastatin: A Review of the Pharmacology and Clinical Effectiveness in Cardiovascular Disease, Clinical Medicine Insights: Cardiology 6 (2012) 17–33. https://doi.org/10.4137/CMC.S4324. [2] K. Balakumar, C.V. Raghavan, N.T. Selvan, R.H. Prasad, S. Abdu, Self nanoemulsifying drug delivery system (SNEDDS) of Rosuvastatin calcium: Design, formulation, bioavailability and pharmacokinetic evaluation, Colloids and Surfaces B: Biointerfaces. 112 (2013) 337–343. http://dx.doi.org/10.1016/j.colsurfb.2013.08.025. [3] S. Elkadi, S. Elsamaligy, S. Al-Suwayeh, H. Mahmoud, The Development of Self-nanoemulsifying Liquisolid Tablets to Improve the Dissolution of Simvastatin, American Association of Pharmaceutical Scientists 18(7) (2017) 2586–2597. https://doi.org/10.1208/s12249-017-0743-z. [4] D. Patel, K.K. Sawant, Self Micro-Emulsifying Drug Delivery System: Formulation Development and Biopharmaceutical Evaluation of Lipophilic Drugs, Current Drug Delivery 6 (2009) 419–424. https://doi.org/10.2174/156720109789000519. [5] S.D. Maurya, R.K.K. Arya, G Rajpal, R.C. Dhakar, Self-micro emulsifying drug delivery systems (SMEDDS): A review on physico-chemical and biopharmaceutical aspects, Journal of Drug Delivery and Therapeutics 7(3) (2017) 55–65. https://doi.org/10.22270/jddt.v7i3.1453.[6] P. Borman, D. Elder, Q2(R1) Validation of analytical procedures: text and methodology, in: A. Teasdale, D. Elder, R.W. Nims (Eds), ICH quality guidelines: an implementation guide, John Wiley & Sons Inc., Hoboken, 2018, pp. 127-166. [7] United States Pharmacopoeia 41, rosuvastatin tablets monograph.          

scholarly journals Development and Validation of an HPLC Method to Quantify Camptothecin in Polymeric Nanocapsule Suspensions

2008 ◽  
Vol 91 (3) ◽  
pp. 551-556 ◽  
Author(s):  
Andra Granada ◽  
Fabio S Murakami ◽  
Tatiane Sartori ◽  
Elenara Lemos-Senna ◽  
Marcos A S Silva
Keyword(s):  
High Performance ◽  
Early Stage ◽  
Current Method ◽  
Entrapment Efficiency ◽  
High Performance Liquid Chromatographic ◽  
Reversed Phase ◽  
Calibration Graph ◽  
Formulation Development ◽  
Relative Standard ◽  
Limit Of Quantitation

Abstract A simple, rapid, and sensitive reversed-phase column high-performance liquid chromatographic method was developed and validated to quantify camptothecin (CPT) in polymeric nanocapsule suspensions. The chromatographic separation was performed on a Supelcosil LC-18 column (15 cm 4.6 mm id, 5 m) using a mobile phase consisting of methanol10 mM KH2PO4 (60 + 40, v/v; pH 2.8) at a flow rate of 1.0 mL/min and ultraviolet detection at 254 nm. The calibration graph was linear from 0.5 to 3.0 g/mL with a correlation coefficient of 0.9979, and the limit of quantitation was 0.35 g/mL. The assay recovery ranged from 97.3 to 105.0. The intraday and interday relative standard deviation values were <5.0. The validation results confirmed that the developed method is specific, linear, accurate, and precise for its intended use. The current method was successfully applied to the evaluation of CPT entrapment efficiency and drug content in polymeric nanocapsule suspensions during the early stage of formulation development.

scholarly journals Application of Design of Expert software for evaluating the influence of formulation variables on the encapsulation efficacy, drug content and particle size of PEO-PPO-PEO/Poly(DL-lactide-co-caprolactone) nanoparticles as carriers for SN-38

2021 ◽  
Author(s):  
Rozafa Koliqi ◽  
Pranvera Breznica ◽  
Arlinda Daka ◽  
Blerina Koshi
Keyword(s):  
Ethylene Oxide ◽  
Water Solubility ◽  
Entrapment Efficiency ◽  
Diffusion Method ◽  
Formulation Development ◽  
Drug Content ◽  
Poly Ethylene Oxide ◽  
Drug Entrapment Efficiency ◽  
Poly Ethylene ◽  
Poly Propylene

Background and aims. Hydrophobic substances are mainly encapsulated into polymer nanocarriers in order to improve their solubility, enable their administration, at the same time to empower targeted tissue or cell specific delivery of the drug using the encapsulating vehicle as targeting and controlled release platform. 7-Ethyl-10-hydroxycamptothecin (SN-38) is an active metabolite of Irinotecan, showing 100- fold to 1000-fold higher effect than Irinotecan, but its clinical use is limited because of its extreme hydrophobicity, as it is practically insoluble in most physiologically compatible and pharmaceutically acceptable solvents. Method. In order to fully exploit the potential of the nanoprecipitation as a method for preparation of Poly(DL-lactide-co-caprolactone)- poly(ethylene oxide) - poly(propylene oxide) - poly(ethylene oxide) (P(DL)LCL/PEO-PPO-PEO) nanoparticles and evaluate the influence of the polymer P(DL)LCL, stabilizing agent PEO-PPO-PEO copolymer (Lutrol F127) and the drug concentration (SN-38) upon drug entrapment efficiency, size and drug content, a D-optimal experimental design for response surface using Design Expert Version 9.0.4.1. software investigation was created and statistically analyzed. Results. We have observed that at higher SN-38 concentration during the preparation procedure (nanoprecipitation, solvent diffusion method), and due to its extremely low water solubility, the drug will start to precipitate as unprotected crystals at a faster pace compared to polymer aggregation, leading to extremely low encapsulation efficacy and waste of the active compound. The most desirable combination of factor settings are SN-38=0.5 mg, Polymer=5mg and F127=4%. Conclusion. This investigation utilizes the design of experiment approach and extends the primary understanding of impact of formulation development of P(DL)LCL/PEO-PPO-PEO nanoparticles as carriers for SN-38.

Optimization of Brinzolamide Loaded Microemulsion using Formulation by Design Approach: Characterization and In-vitro Evaluation

2020 ◽  
Vol 15 (1) ◽  
pp. 37-52 ◽  
Author(s):  
Riyaz Gohil ◽  
Asha Patel ◽  
Tosha Pandya ◽  
Abhay Dharamsi
Keyword(s):  
Zeta Potential ◽  
Droplet Size ◽  
Ternary Phase Diagram ◽  
Effective Means ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Isopropyl Myristate ◽  
Ocular Delivery ◽  
Ocular Irritation

Background: The clinical application of Brinzolamide, a drug used in the treatment of glaucoma is limited due its poor aqueous solubility. Microemulsion based ocular delivery can be an effective means to improve its solubility and in turn the bioavailability. Objective: The main objective of the present work was optimization and characterization of Brinzolamide loaded microemulsion for the treatment of glaucoma. Method: The solubility of Brinzolamide in various oils and surfactants was checked in order to identify components of microemulsion. Pseudo-ternary phase diagram using Prosim software was plotted to identify microemulsion existence area. D-optimal mixture design was used for optimization of microemulsion. The optimized formulation consisted of Isopropyl myristate, Tween-80 and Transcutol-P as surfactant and co-surfactant respectively, and water. The chosen critical responses were droplet size, zeta potential, nepheloturbidimetric unit, and viscosity. Results: The selected optimal composition shows favorable features, such as droplet size (41.69 nm), Zeta potential (-9.496 mV), Viscosity (170.8 cps), Transparency (1.483 NTU) and pH (7.646) that are suitable for ocular delivery. Moreover, a prolonged drug release (78.08 % within 7 hour) was found in in-vitro experiments. By and large the formulation was found to be safe and nonirritant as proven by the ocular irritation study. Conclusion: Our study illustrated potential of Brinzolamide loaded microemulsion for ocular delivery for the treatment of glaucoma.

scholarly journals Formulation development and evaluation of antiacne activity of ethosomal gel prepared using Plumbago zeylanica root extract

2020 ◽  
Vol 11 (4) ◽  
pp. 5511-5516
Author(s):  
Sandhya P ◽  
Snehalata J
Keyword(s):  
Physicochemical Properties ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Root Extract ◽  
Formulation Development ◽  
Plumbago Zeylanica ◽  
Hydroalcoholic Extract ◽  
Drug Content ◽  
And Diffusion ◽  
Gel Formulations

The objective of present research work is, to develop an ethosome, as a carrier system for Plumbago root extract, its incorporation into gel formulations and to characterize the developed gel formulations by estimation of plumbagin content and study of antiacne activity. Roots of Plumbago zeylanica L (Plumbaginaceae) contains Plumbagin and is used for skin infections and intestinal worms. Topical therapy for acne includes comedolytic agents, antibiotics and anti-inflammatory drugs. The excessive use of antibiotics has led to the increased resistance of acne-causing bacteria. In this research work, plumbago roots have been screened for their potential use for the treatment of acne and hydroalcoholic extract of the roots was found to be effective. Seven batches (EF1-EF7) of ethosomes were prepared using soya lecithin (1-3%) and ethanol (10-45%) and the hydroalcoholic extract. The range of entrapment efficiency varied from 17.12 to 80.82%. The ethosomes EF6 having highest entrapment efficiency was incorporated into gel formulation. Carbopol 934P (0.5 -2%) was used to prepare ethosomal gel and evaluated for physicochemical properties, drug content and diffusion characteristics. The pH of the gel was in the range of 6.87 to 7.03. Viscosity was between 5600 - 9800 centipoises. The % drug content was in the range of 95.91% to 100.7%. The ethosome, in their gel formulation, showed good physicochemical properties, drug content and diffusion pattern. The anti-acne activity of F3 showed good zones of inhibition comparable with standard Clindamycin. The present study suggested ethosomal gel as an efficient carrier for plumbago root extract for antiacne activity.

Development and Validation of A Reversed Phase-High Performance Liquid Chromatography Method for the Quantitative Estimation of Ramipril Drug Content from Formulated Dosage Form

2016 ◽  
Vol 6 (3) ◽  
Author(s):  
Raju Chandra ◽  
Manisha Pant ◽  
Harchan Singh ◽  
Deepak Kumar ◽  
Ashwani Sanghi
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
Active Ingredient ◽  
High Performance ◽  
Limit Of Detection ◽  
Quantitative Estimation ◽  
Reversed Phase ◽  
Uv Detector ◽  
Chromatography Method ◽  
Drug Content

A reliable and reproducible reversed-phase high performance liquid chromatography (RP-HPLC) was developed for the quantitative determination of Remipril drug content from marketed bulk tablets. The active ingredient of Remipril separation achieved with C18 column using the methanol water mobile phase in the ratio of 40:60 (v/v). The active ingredient of the drug content quantify with UV detector at 215 nm. The retention time of Remipril is 5.63 min. A good linearity relation (R2=0.999) was obtained between drug concentration and average peak areas. The limit of detection and limit of quantification of the instrument were calculated 0.03 and 0.09 µg/mL, respectively. The accuracy of the method validation was determined 102.72% by recoveries method.

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.

Development and Characterization Colchicine-Loaded PEGylated Gelatin Nanoparticles for Targeted Delivery to Tumor

2013 ◽  
Vol 6 (2) ◽  
pp. 2058-2063
Author(s):  
G D Chandrethiya ◽  
P K Shelat ◽  
M N Zaveri
Keyword(s):  
Drug Delivery ◽  
Targeted Delivery ◽  
High Performance ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Spherical Particles ◽  
Precipitation Method ◽  
Antitumoral Activity ◽  
Gelatin Nanoparticles

PEGylated gelatin nanoparticles loaded with colchicine were prepared by ethanol precipitation method. Poly-(ethylene glycol)-5000-monomethylether (MPEG 5000), a hydrophilic polymer, was used to pegylate gelatin.  Gluteraldehyde was used as cross-linking agent. To obtain a high quality product, major formulation parameters were optimized.  Spherical particles with mean particles of 193 nm were measured by a Malvern particle size analyzer. Entrapment efficiency was found to be 71.7 ± 1.4% and determined with reverse phase high performance liquid charomatography (RP-HPLC). The in vitro drug release study was performed by dialysis bag method for a period of 168 hours. Lyophilizaton study showed sucrose at lower concentrations proved the best cryoprotectant for this formulation.  Stability study revealed that lyophilized nanoparticles were equally effective (p < 0.05) after one year of storage at 2-8°C with ambient humidity. In vitro antitumoral activity was accessed using the MCF-7 cell line by MTT assay.  The IC50 value was found to be 0.034 μg/ml for the prepared formulation. The results indicate that PEGylated gelatin nanoparticles could be utilized as a potential drug delivery for targeted drug delivery of tumors.  

Cationic Diclofenac Lipid Nanoemulsion for Improved Oral Bioavailability: Preparation, Characterization and In Vivo Evaluation

2015 ◽  
Vol 8 (2) ◽  
pp. 2874-2880
Author(s):  
Kishan Veerabrahma ◽  
Swapna Madishetty ◽  
Muzammil Afzal Syed ◽  
Prabhakar Kandadi
Keyword(s):  
Oral Bioavailability ◽  
Physical Stability ◽  
Cationic Lipid ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Pharmacokinetic Parameters ◽  
In Vivo Evaluation ◽  
Drug Content ◽  
Lipid Nanoemulsion

Cationic nanoemulsions were reported to have increased bioavailability. The aim of present study was to prepare a cationic lipid nanoemulsion of diclofenac acid (LNEs) for improved oral bioavailability to treat arthritic conditions. The LNEs of diclofenac acid were prepared by using soya bean oil, egg lecithin, cholesterol and stearylamine. Stearylamine was used as positive charge inducer. The LNEs were processed by homogenization and ultrasonication. The formulation composition was selected based on earlier reports. The LNEs were characterized for size and zeta potential. The physical stability of LNEs was studied using autoclaving, centrifugal, desorption (dilution effect) stresses and on storage. The total drug content and entrapment efficiency were determined using HPLC. During in vivo studies in Wistar rats, the pharmacokinetic parameters of LNEs were compared with a prepared diclofenac suspension in sodium CMC mucilage. The selected formulations, F1, F2 and F3, were relatively stable during centrifugal stress, dilution stress and on storage. The drug content was found to be 2.38 ± 1.70 mg/ml for F1, 2.30 ± 0.82 mg/ml for F2, and 2.45 ± 0.66 mg/ml for F3. The entrapment efficiencies were 97.83 ± 0.53%, 97.87 ± 1.22% and 98.25 ± 0.21% for F1, F2 and F3 respectively. The cumulative percentage drug release from F1, F2 and F3 showed more release in pH 6.8 phosphate buffer than in pH 1.2 HCl. During oral bioavailability studies, the LNEs showed higher serum concentrations than a suspension. The relative bioavailability of the LNE formulations F1, F2 and F3 were found to be 2.35, 2.94 and 6.28 times that of F4 suspension and were statistically significant. Of all, the cationic lipid nanoemulsion (F3) was superior in improving bioavailability, when compared with plain emulsion (F1) and cholesterol containing LNE (F2). The study helps in designing the cationic oral nanoemulsions to improve the oral bioavailability of diclofenac.

scholarly journals Stabilization and Release of Palm Tocotrienol Emulsion Fabricated Using pH-Sensitive Calcium Carbonate

Foods ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 358
Author(s):  
Phui Yee Tan ◽  
Beng Ti Tey ◽  
Eng Seng Chan ◽  
Oi Ming Lai ◽  
Hon Weng Chang ◽  
...  
Keyword(s):  
Calcium Carbonate ◽  
Droplet Size ◽  
Entrapment Efficiency ◽  
Ph Sensitive ◽  
Emulsion System ◽  
Ph Responsive ◽  
Small Droplet ◽  
Homogenization Time ◽  
Oil In Water ◽  
Ph Range

Calcium carbonate (CaCO3) has been utilized as a pH-responsive component in various products. In this present work, palm tocotrienols-rich fraction (TRF) was successfully entrapped in a self-assembled oil-in-water (O/W) emulsion system by using CaCO3 as the stabilizer. The emulsion droplet size, viscosity and tocotrienols entrapment efficiency (EE) were strongly affected by varying the processing (homogenization speed and time) and formulation (CaCO3 and TRF concentrations) parameters. Our findings indicated that the combination of 5000 rpm homogenization speed, 15 min homogenization time, 0.75% CaCO3 concentration and 2% TRF concentration resulted in a high EE of tocotrienols (92.59–99.16%) and small droplet size (18.83 ± 1.36 µm). The resulting emulsion system readily released the entrapped tocotrienols across the pH range tested (pH 1–9); with relatively the highest release observed at pH 3. The current study presents a potential pH-sensitive emulsion system for the entrapment and delivery of palm tocotrienols.

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