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

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.

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Stability Study of Super Saturable Catechin-Self Nano Emulsifying Drug Delivery System as Antidiabetic Therapy

Biointerface Research in Applied Chemistry ◽

10.33263/briac125.58115820 ◽

2021 ◽

Vol 12 (5) ◽

pp. 5811-5820

Keyword(s):

Oxidative Stress ◽

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Tea Plant ◽

Stability Study ◽

Good Stability ◽

Antidiabetic Therapy ◽

Thaw Cycle ◽

The Stability

Diabetes mellitus is a metabolic syndrome characterized by hyperglycemic and increased ROS production, which causes oxidative stress. Catechin isolated from the tea plant has oxidative stress inhibitor activity and anti-diabetic activity with low absorption in circulation systemic. Therefore, it is formulated in a super saturable catechin-self nano emulsifying drug delivery system (SSC-SNEDDS). Stability is one of the factors that affect the safety, quality, and efficacy of SSC-SNEDDS. This study aims to evaluate the stability of the formulated oil phase using oleic acid, croduret as a surfactant, and propylene glycol as a co-surfactant. Stability studies were carried out by several tests, namely heating-cooling cycle assay, freeze-thaw cycle assay, centrifugation, and endurance assay. Droplet characterization in the form of changes in diameter, zeta potential, and mobility in evaluating stability tests using dynamic light scattering-particle size analyzer (DLS-PSA). Real-time stability was also evaluated by observing changes in the infrared spectrum pattern using FTIR-ATR. After the stability test, the emulsion droplet size of SSC-SNEDDS was still below 100 nm and showed good stability. It can be concluded that the formula has a good stability profile.

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FORMULATION DEVELOPMENT AND IN VITRO ANTIOXIDANT AND ANTIDIABETIC EVALUATION OF ERIOBOTRYA JAPONICA BASED SELF NANO EMULSIFYING DRUG DELIVERY SYSTEM

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i4.33006 ◽

2019 ◽

pp. 313-319

Author(s):

AMRIT PAL SINGH ◽

GOPAL L. KHATIK ◽

VIJAY MISHRA ◽

NAVNEET KHURANA ◽

NEHA SHARMA ◽

...

Keyword(s):

Drug Delivery ◽

Zeta Potential ◽

Drug Delivery System ◽

Droplet Size ◽

Delivery System ◽

Methanolic Extract ◽

Tween 80 ◽

Eriobotrya Japonica ◽

Formulation Development

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.

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Self Nano-Emulsifying Drug Delivery System (SNEDDS) of Curcuma Mangga Val. Essential Oil and The Stability Study

INDONESIAN JOURNAL OF PHARMACY ◽

10.22146/ijp.584 ◽

2020 ◽

pp. 238-243

Author(s):

Retno Sunarminingsih Sudibyo ◽

Lukman Mahdi ◽

Ronny Martien

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Essential Oil ◽

Zeta Potential ◽

Drug Delivery System ◽

Droplet Size ◽

Delivery System ◽

Stability Study ◽

Freeze Thaw ◽

Lattice Design

Essential oil of Curcuma mangga Val. has been reported to have cytotoxic effect against cancer cell lines. But this oil is unstable in dispensing so that a self nano-emulsifying drug delivery system (SNEDDS) of the oil was conducted to solve the problem and improve its potency. In the study, optimization, verification, characterization, and stability test of the SNEDDS formula were carried out respectively by simplex lattice design (SLD) on Design Expert ver. 10 software, droplet size and Zeta potential determinations using particle size analyzer (PSA) instrument, as well as heating-cooling and freeze-thaw methods. The best SNEDDS formula resulted was Miglyol : Tween 80 : PEG 400 = 16.034% : 68.380% : 15.586%; with transmittance of 84.47 + 1.05%, droplet size of 15.75 nm, zeta potential of -8.54 mV, polydispersity index (PDI) of 0.188, emulsifying time of 49.67 + 1.7 seconds in distilled water, 24.33 + 4.19 seconds in artificial gastric fluid and 21.33 + 2.87 seconds in artificial intestine fluid. After a freeze-thaw test there was no change on the emulsion’s clarity, color, smell, as well as no separation, which means that the formula was stable thermodynamically. The optimum SNEDDS formula resulted has small particle size, better emulsifying time in artificial gastric and intestine fluids, as well as better thermodynamic stability, which in turn will improve the cytotoxic activity of the Curcuma mangga Val. rhizome oil toward cancer cells.

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Formulation development & Evaluation of Phospholipids Complex of Euphorbia neriifolia Linn Extract

Journal of Biomedical and Pharmaceutical Research ◽

10.32553/jbpr.v10i6.891 ◽

2021 ◽

Vol 10 (6) ◽

Author(s):

Pranay Sethiya ◽

S.C. Mahajan ◽

Prachi Maheshwari ◽

Anjali Khantal ◽

Harshita Sharma

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Molecular Size ◽

Entrapment Efficiency ◽

Lipid Solubility ◽

Formulation Development ◽

Vis Spectroscopy ◽

Novel Drug Delivery System ◽

Novel Drug

Phytoconstituents have been utilized as medicines for thousands of years, yet their application is limited owing to major hurdles like deficit lipid solubility, large molecular size and degradation in the gastric environment of gut. To overcome this hurdle, Novel Drug Delivery System (NDDS) proves to be a promising method for formulations containing phytoconstituents. In present work, phyto-phospholipids complex (phytosomes) of Euphorbia neriifolia L. has been prepared to improve the absorption and bioavailability of phytoconstituents. Euphorbia neriifolia L. consists of flavonoids, saponins and polyphenols which possess various medicinal properties. These constituents are hydrophilic in nature and have large molecular size, thus causing poor absorption. Phyto-phospholipids complex of Euphorbia neriifoliahas been prepared by taking Phosphatidylcholine (PC), Cholesterol and Euphorbia neriifolia extract in different ratio and the formulation been optimized to achieve maximum entrapment efficiency and smaller molecular size. The prepared phytosomes has been evaluated by Optical Microscopy, Transmission Electron Microscopy, Dynamic Light Scattering and UV/Vis Spectroscopy for physical appearance, entrapment efficiency, particle size, zeta potential and dissolution rate. The result so obtained indicates the improvement in the absorption rate and bioavailability of the phytoconstituents. Thus, Novel Drug Delivery System (NDDS) possess a great potential in overcoming the challenges of plant based formulations. Keywords: Euphorbia neriifolia, Phyto-phospholipids Complex, Novel Drug Delivery System, Phytosomes

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