In-Vitro and In-Vivo Evaluation of Supersaturable Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Dutasteride

2020 ◽  
Vol 17 (1) ◽  
pp. 74-86 ◽  
Author(s):  
Poonguzhali Subramanian ◽  
P. S. Rajnikanth ◽  
Manish Kumar ◽  
Kumarappan Chidambram
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Absorption ◽  
Drug Loading ◽  
Methyl Cellulose ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Drug Load

Objective: A novel, Supersaturable Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) has been prepared to improve the Dutasteride's poor aqueous solubility. Methods: By adding Hydroxy Propyl Methyl Cellulose (HPMC) as a precipitation inhibitor to conventional SNEDDS, a supersaturable system was prepared. Firstly, the prepared SNEDDS played an important role in increasing the aqueous solubility and hence oral absorption due to nano-range size. Secondly, the S-SNEDDS found to be advantageous over SNEDDS for having a higher drug load and inhibition of dilution precipitation of Dutasteride. Formulated S-SNEDDS (F1-F9) ranged from 37.42 ± 1.02 to 68.92 ± 0.09 nm with PDI 0.219-0.34 and drug loading of over 95 percent. Results: The study of in-vitro dissolution revealed higher dissolution for S-SNEDDS compared to SNEDDS and Avodart soft gelatin capsule as a commercial product. In addition, higher absorption was observed for S-SNEDDS showing approximately 1.28 and 1.27 fold AUC (0-24h) and Cmax compared to commercial products. Therefore, S-SNEDDS has proven as a novel drug delivery system with a higher drug load, higher self-emulsification efficiency, higher stability, higher dissolution and pronounced absorption. Conclusion: In conclusion, S-SNEDDS could be a new emerging approach to enhance aqueous solubility in many folds for drugs belonging to BCS Class II and IV and thus absorption and oral bioavailability.

scholarly journals FORMULATION AND EVALUATION OF SOLID SELF-EMULSIFYING DRUG DELIVERY SYSTEM OF GLICLAZIDE

2016 ◽  
Vol 8 (11) ◽  
pp. 144
Author(s):  
Suwarna R. Deshmukh ◽  
Suparna S. Bakhle ◽  
Kanchan P. Upadhye ◽  
Gouri R. Dixit
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Water Soluble Drug

Objective: Gliclazide (GCZ) is a widely prescribed anti-diabetic drug belongs to class IΙ under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. The present investigations highlight the development of solid self-emulsifying drug delivery system (solid-SEDDS) for improved oral delivery of the poorly water-soluble drug, GCZ.Methods: Various oils, surfactant and co-surfactant, were screened for their emulsification ability. Ternary phase diagrams were plotted to identify the zone of micro-emulsification. Liquid SEDDS of the drug were formulated using lemon oil as the oil phase, tween 80, as the surfactant, and labrasol, as the co-surfactant. The optimized liquid SEDDS was transformed into free-flowing powder using florite R as the adsorbent. Results: Self-emulsifying powder retained the self-emulsifying property of the liquid SEDDS. The morphology of solid-SEDDS from scanning electron microscopy studies demonstrated the presence of spherical, granular particles indicating good flowing ability. X-ray powder diffraction studies confirmed solubilization of the drug in the lipid excipients and/or transformation of a crystalline form of the drug to amorphous form. In vitro dissolution studies revealed enhanced release of the drug from solid-SEDDS as compared to plain drug and marketed formulation.Conclusion: Thus it can be concluded that solid-SEDDS, amenable for the development of solid dosage form, can be successfully developed using florite R with the potential of enhancing the solubility, dissolution rate, and bioavailability of the drug.

scholarly journals Applicability of Gum Karaya in the Preparation and in Vitro Evaluation of Losartan Potassium as Chronotherapeutic Drug Delivery System

2015 ◽  
Vol 7 (1-2) ◽  
pp. 65-74
Author(s):  
K. Latha ◽  
V. V. Srikanth ◽  
S. A. Sunil ◽  
N. R. Srinivasa ◽  
M. U. Uhumwangho ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Tensile Strength ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lag Time ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Burst Release ◽  
Gum Karaya

The objective of this investigation is to study the applicability of gum karaya, the natural gum for the preparation and in vitro evaluation of losartan potassium, as Chronotherapeutic Drug Delivery System (ChDDS). The compression-coated timed-release tablets (CCT) containing losartan potassium in the core tablet were prepared by dry coating technique with different ratios of gum karaya as the outer coat. The parameters investigated were tensile strength, friability, in vitro dissolution studies and drug concentration. The optimized formulation was further characterized by powder XRD and FTIR to investigate interactions and no interactions observed. The tensile strength and friability of all the CCT were between 1.06-1.23 MN/m2 and < 0.3% respectively.  All the CCT showed a clear lag time before a burst release of drug. However, the lag time of drug release increased as the amount of gum karaya in the outer layer increased. For instance, the lag time of LGK1, LGK2, LGK3, LGK4, LGK5, LGK6 and LGK7 were 16, 10.5, 5.5, 3, 2, 1.5 and 0.5 hrs respectively.  The drug content of all the CCT was >98%. Formulation LGK3 was taken as an optimized formulation which can be exploited to achieve ChDDS of losartan potassium for the treatment of hypertension. 

A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems

2021 ◽  
Vol 14 (4) ◽  
pp. 5519-5228
Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
Particle Size Reduction

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.  

A Smart Drug Delivery System Based on Thermo-Responsive Polymer Gated Au NRs@SiO2 Nano-Platform

2021 ◽  
Vol 16 (7) ◽  
pp. 1029-1036
Author(s):  
Hongzhu Wang ◽  
Mengxun Chen ◽  
Liping Song ◽  
Youju Huang
Keyword(s):  
Drug Delivery ◽  
Block Copolymer ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Photothermal Therapy ◽  
Drug Loading ◽  
Temperature Sensitive

A key challenge for nanoparticles-based drug delivery system is to achieve manageable drug release in tumour cell. In this study, a versatile system combining photothermal therapy and controllable drug release for tumour cells using temperature-sensitive block copolymer coupled Au NRs@SiO2 is reported. While the Au NRs serve as hyperthermal agent and the mesoporous silica was used to improve the drug loading and decrease biotoxicity. The block copolymer acted as “gatekeeper” to regulate the release of model drug (Doxorubicin hydrochloride, DOX). Through in vivo and in vitro experiments, we achieved the truly controllable drug release and photothermal therapy with the collaborative effect of the three constituents of the nanocomposites. The reported nanocomposites pave the way to high-performance controllable drug release and photothermal therapy system.

SELF-EMULSIFYING DRUG DELIVERY SYSTEM CONTAINING ACECLOFENAC: DESIGN & DEVELOPMENT USING QUALITY BY DESIGN (QBD) CONCEPT

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (06) ◽  
pp. 16-26
Author(s):  
V Suthar ◽  
◽  
M Gokel ◽  
S Butani ◽  
A Solanki
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Dosage Form ◽  
Quality By Design ◽  
Tween 80 ◽  
Current Approach ◽  
In Vitro Dissolution ◽  
Design Development

The aim of the present study was to develop self-emulsifying drug delivery system (SEDDS) of aceclofenac for potential improvement in the in vitro dissolution. The Food and Drug Control Agency (FDCA) has put more stress on the quality, safety and efficacy of the dosage form. The use of design of experiments and quality by Design (QbD) in the development of self emulsifying drug delivery system (SEDDS) containing aceclofenac is demonstrated. The optimum formulation contained Labrafil M 1944 CS, Tween 80 and Transcutol P. The systematic approach enabled us in identifying the design space. The results revealed that while devising the control strategies during manufacturing, more attention should be focused on the ratios of oil to surfactant and surfactant to co-surfactant. The drug was released at a faster rate due to a large surface area. The current approach enabled us to develop a dosage form which is economic, patient-friendly and does not require assistance of a doctor or nurse, especially at remote places at odd hours.

DEVELOPMENT AND EVALUATION OF ZIPRASIDONE LOADED SOLID SELF-MICRO EMULSIFYING DRUG DELIVERY SYSTEM

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (08) ◽  
pp. 53-60
Author(s):  
Purushottam Patil ◽  
Malik Shaikh ◽  
Paresh Mahaparale
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Physical Adsorption ◽  
Gastrointestinal Transit ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Poorly Water Soluble

Solid self-micro emulsification technique is the new approach for poorly water-soluble and poorly bioavailable drugs by allowing the drug substance to be incorporated into the oil phase and thus having the ability to permeate the GI membrane to a faster extent. Oleic acid, Tween 80, methanol and colloidal silicon dioxide were used as penetrant, surfactant, co-surfactant and adsorbent, respectively. The interaction between drug and excipients was examined by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The results of DSC and FTIR studies did not reveal any possible drug-excipient interactions. The conversion of liquid self-microemulsifying drug delivery system (SMEDDS) into the solid SMEDDS increases the stability of the emulsion formulation achieved by physical adsorption of an adsorbent material. The release of drug from SMEDDS formulation is justified by in-vitro dissolution studies. SMEDDS increases the solubility of the drug and improves the bioavailability, without disturbing gastrointestinal transit. SMEDDS has the potential to provide a useful oral solid dosage form for the poorly water-soluble drug ziprasidone.

scholarly journals In Vitro Cytotoxicity and Antitumor Activity of Dual-Targeting Drug Delivery System Based on Modified Magnetic Carbon by Folate

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Jinglei Du ◽  
Qiang Li ◽  
Lin Chen ◽  
Shicai Wang ◽  
Li Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Hela Cells ◽  
Folate Receptor ◽  
Drug Loading ◽  
Magnetic Characteristics ◽  
Loading Capacity ◽  
Dual Targeting

A dual-targeting drug delivery system (DTDDS) with magnetic targeting and active targeting was obtained to improve the targeting and drug-loading capacity of magnetic drug nanocarriers. An ultraviolet-visible spectrophotometer and flow cytometry were used to investigate the drug-loading and release capacity, cytotoxicity, and inhibition of tumor cell proliferation, separately. Results show that DTDDS has obvious magnetic characteristics, on which the modification amount of folic acid is 64.82 mg g-1. Doxorubicin was taken as a template drug to evaluate its drug-loading capacity, which was as high as 577.12 mg g-1. Good biocompatibility and low cytotoxicity of DTDDS were further confirmed. Moreover, DTDDS can target the folate receptor on the surface of HeLa cells and deliver doxorubicin into HeLa cells, thereby increasing the proliferation inhibition for cancer cells. Therefore, this new dual-targeting drug delivery system shows potential in significantly reducing the toxic side effects of chemotherapy and improving chemotherapy efficiency.

Enhanced Oral Bioavailability and Improved Biological Activities of a Quercetin/Resveratrol Combination Using a Liquid Self-Microemulsifying Drug Delivery System

Planta Medica ◽  
2020 ◽  
Author(s):  
Patcharawalai Jaisamut ◽  
Subhaphorn Wanna ◽  
Surasak Limsuwan ◽  
Sasitorn Chusri ◽  
Kamonthip Wiwattanawongsa ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Biological Activities ◽  
Area Under The Curve ◽  
Aqueous Solubility ◽  
The Self

AbstractBoth quercetin and resveratrol are promising plant-derived compounds with various well-described biological activities; however, they are categorized as having low aqueous solubility and labile natural compounds. The purpose of the present study was to propose a drug delivery system to enhance the oral bioavailability of combined quercetin and resveratrol. The suitable self-microemulsifying formulation containing quercetin together with resveratrol comprised 100 mg Capryol 90, 700 mg Cremophor EL, 200 mg Labrasol, 20 mg quercetin, and 20 mg resveratrol, which gave a particle size of 16.91 ± 0.08 nm and was stable under both intermediate and accelerated storage conditions for 12 months. The percentages of release for quercetin and resveratrol in the self-microemulsifying formulation were 75.88 ± 1.44 and 86.32 ± 2.32%, respectively, at 30 min. In rats, an in vivo pharmacokinetics study revealed that the area under the curve of the self-microemulsifying formulation containing quercetin and resveratrol increased approximately ninefold for quercetin and threefold for resveratrol compared with the unformulated compounds. Moreover, the self-microemulsifying formulation containing quercetin and resveratrol slightly enhanced the in vitro antioxidant and cytotoxic effects on AGS, Caco-2, and HT-29 cells. These findings demonstrate that the self-microemulsifying formulation containing quercetin and resveratrol could successfully enhance the oral bioavailability of the combination of quercetin and resveratrol without interfering with their biological activities. These results provide valuable information for more in-depth research into the utilization of combined quercetin and resveratrol.

scholarly journals SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEM OF EFAVIRENZ: FORMULATION, IN VITRO EVALUATION AND CHARACTERIZATION

2019 ◽  
pp. 217-226
Author(s):  
PAMU SANDHYA
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Release ◽  
Visual Observation ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Tween 20

Objective: The main objective of this study was to preparation and evaluation of efavirenz (EFV) to enhance its solubility and dissolution rate by self-emulsifying drug delivery system. Methods: EFV self-emulsifying drug delivery systems (SNEDDS) were formulated using different oils, surfactant, and co-surfactant. Peceol, Tween 20, and Capmul MCM were used as oil, surfactant, and co-surfactant, respectively, followed by the evaluation by the performance of different tests such as visual observation, solubility studies, thermodynamic stability study, transmittance studies, drug content, and in-vitro release study. Results: Fourier-transform infrared studies revealed negligible drug and polymer interaction. From the phase diagram, it was observed that self-emulsifying region was enhanced with increasing surfactant and co-surfactant concentrations with oil. F13 was selected as optimized formulation on the basis of physicochemical parameters, particle size, and in-vitro dissolution studies with the release of 98.39±5.10% drug in 1 hour. The optimized formulation size was found to be 156.7 nm as mean droplet size and Z-Average of 808.6 nm with -18.3 mV as zeta potential. Conclusion: The study demonstrated that SNEDDS was a promising strategy to enhance the dissolution rate of EFV by improving solubility.

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