Formulation Development and Evaluation of Transfero-somes Nano Gel Loaded with Levocetirizine Transfero-somes

Author(s):  
Mounika S Bharath ◽  
Bhushan R Rane ◽  
Ashish S Jain

A new drug delivery technology called transferosomes were came into existence which is an artificial vesicle designed to show the characteristics of a cell vesicle suitable for controlled and potentially directed drug delivery. Transferosome is a highly flexible and stress- responsive compound, complex compound and highly deformed vesicle with an aqueous core surrounded by the complex lipid bilayer thus enabling it to deliver both hydrophilic and hydrophobic drug. Urticaria is a general condition distinguished as brief erythematous and oedematous plaques or papules with defined erythematous borders and central clearing, identified as hives/wheals. Levocetirizine which is used for the treatment is a H1 anti histamine that is actively used in treatment of urticaria. The aim of the present research work was to investigate the potential of transferosome formulations for transdermal delivery of  levocetirizine. The transferosomes were formulated by lipid film hydration technique using Rotary vacuum Evaporator. In the present work levocetirizine vesicle was efficaciously formulated using an appropriate ratio of tween 80 and soya lecithin and was incorporated into gel since gel formulations are easy to administer and patient compliance. Levocetirizine transferosomes was evaluated for vesicle characteristicslike zeta potential, poly-dispersibility index, TEM, and stability study. Theaverage sizes of transferosome were found to be 566.6nm and poly dispersity index (PI) was found to be 0.532, zeta potential of the transferosome was found to be -2.3 mV which indicates that transferosome formulation is stable. Levocetirizine gel was prepared by using various concentrations of Carbopol 934 and is evaluated for their gel characteristics like pH, viscosity, Spreadability, extrudability, homogeneity, drug content, diffusion etc. Gel containing 2% Carbopol show best and promising results. Levocetirizine transferosomal gel were efficaciously formulated by utilizing levocetirizine transferosome which was prepared by thin film hydration method by using soya lecithin and tween 80 in the ratio 85:15. Other Oral formulation used in treatment for urticaria have disadvantage like poor bioavailability, 1st pass metabolism, patient non-compliance etc. Transferosome nano gel loaded with levocetirizine transferosome was found to be more effective than other oral formulations used in treatment for urticaria since transferosome are capable of passing through lipid layer and delivering drug into systemic circulation with maximum bioavailability.

Author(s):  
AMRIT PAL SINGH ◽  
GOPAL L. KHATIK ◽  
VIJAY MISHRA ◽  
NAVNEET KHURANA ◽  
NEHA SHARMA ◽  
...  

Objective: The aim of the present study was to develop and characterize self-nano emulsifying drug delivery system (SNEDDS) of methanolic extract of Eriobotrya japonica (Thunb.) Lindl. (E. japonica) leaves. Further in vitro antioxidant and antidiabetic potential of an optimized batch of SNEDDS was explored. Methods: Oil (Labrafil M 1944 CS), surfactant (Tween 80) and co-surfactant (Transcutol P) were selected on the basis of solubility of the methanolic extract. Twenty-seven batches of SNEDDS were prepared with different compositions of oil, surfactant and co-surfactant. The optimized batch was evaluated for its entrapment efficiency, droplet size, polydispersity index (PDI), zeta potential, transmission electron microscopy (TEM). Further, DPPH assay and α-amylase activity were also performed to check the antioxidant and antidiabetic potential of prepared SNEDDS. Results: The optimized design suggested that 10% of Labrafil M 1944CS, 30% of Tween 80 and 60% of Transcutol P could develop SNEDDS with 208 nm mean droplet size, 99.64% drug loading, 0.156 PDI and-6 mV zeta potential. TEM image confirmed the droplet size less than 100 nm and the spherical shape of SNEDDS. In vitro antioxidant and antidiabetic activities of SNEDDS revealed the increased efficacy as compared to that of the ascorbic acid and acarbose, respectively. Conclusion: The optimized batch of SNEDDS was found to improve the antioxidant and antidiabetic efficacy of methanolic extract of E. japonica.


Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.


Author(s):  
Phan Thi Nghia ◽  
Tran Thi Hai Yen ◽  
Vu Thi Thu Giang

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.          


2013 ◽  
Vol 749 ◽  
pp. 423-428
Author(s):  
Margarida Rosa Franco ◽  
Tânia Filipa Viana ◽  
Sara Biscaia ◽  
Paulo Bártolo

Parkinsons Disease (PD) is the second most common progressive neurodegenerative disorder and is referred as a leading cause of neurologic disability. The symptoms and signs of PD result from a decrease of dopamines level in the basal ganglia. Accordingly to this, exogenous substitution with dopamine agonists like levodopa, is used to correct the mechanical disorders at the early stages of the disease. Levodopa is referred as a standard in the treatment of PD. The modern studies of PD drug development and experimental therapeutics focuses on the concept of slowing and targeting the release of levodopa to prolong the therapeutic effect and reduce the number of administrations. The transdermal route was thought to be the best route for providing a progressive supply of levodopa to the systemic circulation. Alginate was chosen as a drug carrier because of its biocompatible and biodegradable properties and also because it has been widely used in drug delivery systems (DDS). The aim of this research work was to produce alginate membranes with and without levodopa. A solvent casting based methodology was used. Calcium chloride was assayed as crosslinking agent. Membranes were characterized using Differential Scanning Calorimetry (DSC) techniques. Drug release was evaluated using UV Spectrophotometry.


2012 ◽  
Vol 62 (4) ◽  
pp. 563-580 ◽  

The aim of the study was to develop and evaluate a self- -emulsifying drug delivery system (SEDDS) formulation to improve solubility and dissolution and to enhance systemic exposure of a BCS class II anthelmetic drug, albendazole (ABZ). In the present study, solubility of ABZ was determined in various oils, surfactants and co-surfactants to identify the microemulsion components. Pseudoternary phase diagrams were plotted to identify the microemulsification existence area. SEDDS formulation of ABZ was prepared using oil (Labrafac Lipopfile WL1349) and a surfactant/ co-surfactant (Tween 80/PEG 400) mixture and was characterized by appropriate studies, viz., microemulsifying properties, droplet size measurement, in vitro dissolution, etc. Finally, PK of the ABZ SEDDS formulation was performed on rats in parallel with suspension formulation. It was concluded that the SEDDS formulation approach can be used to improve the dissolution and systemic exposure of poorly water-soluble drugs such as ABZ.


2021 ◽  
Vol 33 (9) ◽  
pp. 2182-2190
Author(s):  
Sabitri Bindhani ◽  
Snehamayee Mohapatra ◽  
Rajat Kumar Kar

This study was planned to increase the intestinal permeability and thereby bioavailability of eprosartan mesylate (EPM) by designing a self-microemulsifying drug delivery system (SMEDDS) by the use of vegetable oils. Various SMEDDS-based formulations were prepared with oleic acid and peppermint oil. Tween 80 was used as surfactant and PEG 400 as co-surfactant. Pseudo ternary phase diagrams were constructed for identifying emulsification region between 1:1, 1:2, 2:1, 3:1 ratio of SCOS mix. Eight batches of SMEDDS were found to be thermodynamically stable and from which SMEDDSOF9 and PF5 were best formulations due to their highest drug content, minimum particle size. They have shown highest release of drug in vitro and higher in vitro drug diffusion and ex vivo permeation analysis than pure drug. FTIR study ascertained no incompatibility between drug and excipients present in formulation. From the accelerated stability study, slight effect on particle size and zeta potential, assay content along with cumulative % of drug release was found. The results demonstrated the SMEDDS of EPM are potent drug delivery system to increase dissolution rate and bioavailability of drug via increased intestinal permeability and consequently improving the therapeutic efficacy of eprosartan mesylate.


2020 ◽  
Vol 10 (4-s) ◽  
pp. 100-107
Author(s):  
Kunjan Gandhi ◽  
Sunil Kumar Shah ◽  
C K Tyagi ◽  
Prabhakar Budholiya ◽  
Harish Pandey

The present research work was carried out to Formulate and evaluation of bilayer tablet dosage form for the treatment of Hypertension.The objective of this study to compare the specific characteristics of Metoprolol [beta selective (cardio selective) adrenoreceptor blocking agent] and Hydrochlorothiazide (Thiazide Diuretics]) in order to design stable formulation. It can be concluded that bilayer tablet were successfully formulated to achieve immediate release of Hydrochlorothiazide (HCTZ)  and tailored release of Metoprolol (MPL)by using Dual Release Drug Absorption System(DUREDAS technology).Both drugs were found to be stable in Bilayer tablet formulation and were found to be stable for few months. This bilayer tablet dosage form increases the stability which may reduce loss and cost of formulation. It improves the benefits of producer, retailer, and patients. Recently, greater attention has been focused on development of bilayer tablet formulations. Over the past 30 years, the expenses and complications involved in marketing new drug entities have increased with concomitant recognition of therapeutic advantages of conventional drug delivery system. Several pharmaceutical companies are currently developing bi-layer tablets, for a variety of reasons: patent extension, efficient pharmacological effect, better patient compliance, etc. Bilayer tablet is becoming new approach for the successful drug delivery system and for better stability in combination. Bilayer tablets can be primary option to avoid chemical incompatibilities between APIs by physical separation. Keywords: Bilayer tablet, DUREDAS Technology, Antihypertensive, Metoprolol, Hydrochlorthiazide


Author(s):  
Vishal N Kushare ◽  
Saravanan S

The goal of this research was to formulate and test invitro the self-nano emulsifying drug delivery system (SNEDDS) of poorly water-soluble herbal material. Linalool, an essential of Coriandrum sativum with anti-epileptic activity, was isolated from Coriandrum sativum by using Soxhlet extraction method followed by column chromatography and fractionates are concentrated under reduced pressure by using rotary flash evaporator. It is low water soluble material; unpredictable dissolution and low bioavailability make it very difficult to administer linalool orally.The captex-200 oil was exhibited maximum solubility of linalool. Thus, it was chosen as the oil phase, while Tween 80 and PEG-200 were chosen as surfactant and co-surfactant respectively for the preparation of linalool SNEDDS. For the determination of existence zone of nanoemulsion, pseudo ternary phase diagram was developed using the Prism Software by using water titration method. Self-nanoemulsion are evaluated for scanning electron microscopy (SEM), particle size analysis, polydispersity index, zeta potential and invitro drug release.The s9 formulation showed 97.72% cumulative release higher than other selected formulations(S4-S8). The S9 formulation showed promising result on droplet size, zeta potential, polydispersity index, invitro drug dissolution. It was concluded that SNEDDS formation from captex-200, tween 80, PEG-200, Smix (4:1), is a promising approach to enhancing substance solubility and the pace of dissolution.


2020 ◽  
Vol 25 (2) ◽  
pp. 81
Author(s):  
Anif Nur Artanti ◽  
Fea Prihapsara ◽  
Dian Eka Ermawati ◽  
Aprilia Saefanan Shofa

Soursop leaf chloroform extract has anticancer activity.  The active ingredient of soursop leaf was acetogenin polypoid derivatives that have a lipophilic characteristic, and less effective to achieve action targets of drugs in biological systems. The Self-Micro Emulsifying Drug Delivery System (SMEDDS) was an effective drug delivery technique that increases the solubility of lipophilic drugs. This study aims to determine the proportion of optimum SMEDDS formula using Simplex Lattice Design (SLD) method. The Formula of SMEDDS was prepared using a combination of Tween 80-Croduret, Propylene Glycol, and Candlenut oil. Optimization formula with SLD method using Design-Expert software based on physical stability parameters there are the percent of transmittance and emulsification time. The optimum formula of SMEDDS was compared with SLD prediction formula using a statistical analysis t-test, then test of loading dose extract, stability test accelerated by centrifugation, particle size, and zeta potential. The proportion of optimum composition of Tween 80-Croduret, Propylene Glycol, and Candlenut oil of SMEDDS was 60.87%; 24.13%; 15.00% respectively. Results of transmittance 41.14±3.78% and emulsification time 119.0±2.08 seconds. The predicted SLD value for the transmittance percent was 55.0% and the emulsification time was 119.59 seconds. The result of the statistical analysis of one sample t-test showed no significant difference between observation results and SLD prediction. The SMEDDS system has F value of 0.99 and capable to load 25.0 mg chloroform extract of soursop leaf each system with an average particle size of 440 nm and zeta potential of +21.5 mV. 


2020 ◽  
Vol 11 (2) ◽  
pp. 9097-9112

The present investigation is aimed to prepare and evaluate the micro emulsion-based phase transition ocular system for delivery of Timolol maleate in the treatment of glaucoma. Timolol maleate is used in the first line of treatment in open-angle glaucoma, belonging to BCS class-I having good solubility and permeability. The rapid precorneal elimination of conventional formulation containing class I drugs exhibits poor therapeutic effect and bioavailability. So, microemulsion (ME) based phase transition systems were formulated and characterized. ME based phase transition system was formulated using Ethyl oleate as oil and CremophorEL as a surfactant, Span 20 as Co-surfactant, and Sorbic acid as a preservative. These systems undergo a phase transition from water-in-oil (w/o) ME to liquid crystalline (LC) state and to coarse emulsion (EM) with a change in viscosity depending on dilution with tear fluid & water content. Prepared microemulsions were characterized for average globule size, zeta potential, pH, conductance, in-vitro gelling capacity. The optimized formulation was selected based on desirable attributes and was further characterized and compared with marketed ophthalmic gel-forming marketed solution of Timolol maleate (TIMOPTIC-XE®). All the results of the characterization were satisfactory. The optimized water-in-oil (w/o) microemulsion showed droplet size 23.47 nm, the zeta potential of 0.253mV, pH of 7.2, the conductance of 0.25mS, and drug content of 99.64%. The phase transition w/o ME provides the fluidity for installation with its viscosity being increased due to phase transition after application increasing ocular retention while retaining the therapeutic efficiency. The in- vitro drug release and IOP reduction with optimized formulation were found comparable and less fluctuating compared to marketed formulation. Optimized formulation was found stable during the accelerated stability study. The developed phase transition w/o ME formulation would be able to offer benefits, such as increased residence time, prolonged drug release, reduction in dosing frequency, and thereby it will improve patient compliance.


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