A Systemic Review on the Self Micro Emulsifying Drug Delivery System

Comfort direction and painless method made oral route the most favored. Mainstream of recent active constituents have less oral bioavailability because of dissolution rate limited absorption. While many inventive methods like complexation, cocrystals exist, solid dispersions, pH modification and, lipid-based delivery systems conclusively improved appliance with the seeming rise in drug absorption. Among lipid-based formulations, self-micro emulsifying formulations (SMEDDS) (droplet size < 100 nm) are evident to enhance permeation across intestinal membrane, protection of drug against gastric effect, unit dosage is possible, increased bioavailability of drug, reduces the dose of drug etc. Numerous components are used to formulate these dosage forms like Oil, surfactants, Co-surfactant and lipids mixture contribute to the enhancement in oral bioavailability through promoting the lymphatic passage; thus, hepatic first pass metabolism can be overcoming. The present review highlights comprehensive information on the formulation design, probable mechanisms and characterization of SMEDDS

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Frontispiz: Glyceride-Mimetic Prodrugs Incorporating Self-Immolative Spacers Promote Lymphatic Transport, Avoid First-Pass Metabolism, and Enhance Oral Bioavailability

Angewandte Chemie ◽

10.1002/ange.201684461 ◽

2016 ◽

Vol 128 (44) ◽

Author(s):

Luojuan Hu ◽

Tim Quach ◽

Sifei Han ◽

Shea F. Lim ◽

Preeti Yadav ◽

...

Keyword(s):

Oral Bioavailability ◽

Lymphatic Transport ◽

First Pass Metabolism ◽

First Pass ◽

Pass Metabolism

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FORMULATION AND CHARACTERIZATION OF TOPICAL NANO EMULGEL OF TERBINAFINE

Universal Journal of Pharmaceutical Research ◽

10.22270/ujpr.v3i6.223 ◽

2019 ◽

Author(s):

Sonia Paliwal ◽

Gurleen Kaur

Keyword(s):

Phase Diagram ◽

Gelling Agent ◽

Distilled Water ◽

Physiochemical Properties ◽

Dosing Frequency ◽

First Pass Metabolism ◽

First Pass ◽

The Stability ◽

Pass Metabolism

Terbinafine is a broad spectrum antifungal drug. The aim of present study was to develop topical nano emulgel of terbinafine using carbopol 934 as a gelling agent. The objective behind the formulation was to avoid dosing frequency and to increase the stability and bioavailability by avoiding the first pass metabolism. The formulations were prepared by using oleic acid, carbopol 934, span 20, propylene glycol in different ratios and analyzed by pseudo tertiary phase diagram. All the five prepared nano emulgel formulations have shown satisfactory physiochemical properties. The stability and particle size is been determined by zeta potential. The highest drug release 82.38 %was found in formulations of batch F4, which follows non-fickian mechanism. The studies showed that changing the concentration of oil, surfactant, co surfactant and double distilled water as aqueous phase has an impact on the behavior and thermodynamic stability of the nanoemulsion. Study concludes that of Terbinafine can be deliverered effectively by nano emulgel formulations.

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DESIGN AND CHARACTERIZATION OF NOVEL EMULGEL FOR PAIN MANAGEMENT

INDIAN DRUGS ◽

10.53879/id.53.10.10596 ◽

2016 ◽

Vol 53 (10) ◽

pp. 16-20

Author(s):

S. S Magdum ◽

◽

P.S Dounde ◽

D. D. Kamble ◽

S. V.* Patil ◽

...

Keyword(s):

Penetration Enhancers ◽

Gelling Agent ◽

Hydrophobic Drugs ◽

Hydrophilic Drugs ◽

First Pass Metabolism ◽

First Pass ◽

Formulation Parameters ◽

Gi Absorption ◽

Pass Metabolism

Topical DDS is a localized system preferred for drugs having hurdles like first pass metabolism through gastro intestinal absorption, reduced bioavailability, relatively short residence time and dose dumping. To provide continuous percutaneous absorption of drug at controlled rate which overcomes problems associated with GI absorption for oral DDS, semisolid formulations like cream, ointment and gel were preferred in topical DDS applied on skin. Amongst them gels having more aqueous portion have greater dissolution of drug. But these properties are suitable for hydrophilic drugs and not for hydrophobic drugs. This problem was solved by formulating an emulgel in which hydrophobic drugs can be incorporated in gel and used for topical application. The aim of this work was to develop emulgel of acelofenac a hydrophobic drug using Carbapol 940 as gelling agent and clove oil and mentha oil as penetration enhancers. Another aim was to investigate effect of concentration and formulation parameters on spreading coefficient drug release and viscosity of prepared emulgel.

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Development and Optimization of Mirabegron of Solid Lipid Nanoparticles as an Oral Delivery for Overactive Bladder

Pharmaceutical Nanotechnology ◽

10.2174/2211738509666210127143107 ◽

2021 ◽

Vol 09 ◽

Author(s):

Prajakta Raut ◽

Makarand Gambhire ◽

Dhruvi Panchal ◽

Vaishali Gambhire

Keyword(s):

Overactive Bladder ◽

Solid Lipid Nanoparticles ◽

Oral Bioavailability ◽

Lipid Nanoparticles ◽

Correlation Spectroscopy ◽

Solid Lipid ◽

Peg 400 ◽

First Pass Metabolism ◽

First Pass ◽

Pass Metabolism

Background: Mirabegron (MBN), a β-3 adrenergic agent, is used in the treatment of overactive bladder. MBN has alow water solubility, high first-pass metabolism, and low bioavailability, consequently, having poor absorption in the gastrointestinal tract. Objective: The present study is intended at formulating Mirabegron-loaded solid lipid nanoparticles (MBN-SLN) coated with PEG-400 to bypass hepatic first-pass metabolism and to improve its oral bioavailability. Methods: MBN-SLNs were developed using glyceryl monostearate by pre-emulsion- ultrasonication method which was then optimized applying Box-Behnken Design. The optimized batch of MBN-SLN was selected for surface-modification with PEG-400 (MBN-PEG-SLN) and characterized by photon correlation spectroscopy, DSC, and XRD. Bioavailability studies were conducted in Wistar rats after oral administration of plain MBN dispersion, MBN-SLN, and MBN-PEG-SLN. Results: Stable MBN-SLNs and MBN-PEG-SLN of the optimized batch having a mean particle size of 162.7 nm and 149.9 nm; Zeta potential of -39.1 mV and -30.9 mV; %entrapment of 89.90% and 90.12%, respectively, were developed. The results of the in-vitro drug release studies demonstrated a significant slow release of MBN from MBN-SLN (69.38%) and MBN-PEG-SLN (61.33%) as compared to the dispersion of pure drug (92.10%). The relative bioavailability, as a result of the invivostudies, of MBN from MBN-PEG-SLN increased by 2-fold, based on the Cmax values, in comparison with the plain MBN dispersion. Conclusion: Thus, the study established that the oral bioavailability of MBN could be improved by the administration of MBN-PEG-SLN. The obtained results indicate SLNs as a potential drug delivery system for improving the bioavailability of poorly bioavailable drugs such as MBN by abating the first-pass metabolism.

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Reduction of oral bioavailability of lignocaine by induction of first pass metabolism in epileptic patients.

British Journal of Clinical Pharmacology ◽

10.1111/j.1365-2125.1979.tb05904.x ◽

1979 ◽

Vol 8 (1) ◽

pp. 21-31 ◽

Cited By ~ 35

Author(s):

E. Perucca ◽

A. Richens

Keyword(s):

Oral Bioavailability ◽

First Pass Metabolism ◽

First Pass ◽

Epileptic Patients ◽

Pass Metabolism

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Preclinical Pharmacokinetic Evaluation of β-Lapachone: Characteristics of Oral Bioavailability and First-Pass Metabolism in Rats

Biomolecules & Therapeutics ◽

10.4062/biomolther.2015.029 ◽

2015 ◽

Vol 23 (3) ◽

pp. 296-300 ◽

Cited By ~ 10

Author(s):

Iksoo Kim ◽

Hyeongmin Kim ◽

Jieun Ro ◽

Kanghee Jo ◽

Sandeep Karki ◽

...

Keyword(s):

Oral Bioavailability ◽

First Pass Metabolism ◽

First Pass ◽

Pass Metabolism ◽

Pharmacokinetic Evaluation

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Solid lipid nanocarriers as alternative drug delivery system for improved oral delivery of drugs

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v10i6-s.4410 ◽

2020 ◽

Vol 10 (6-s) ◽

pp. 168-172

Author(s):

Gorre Thirupathi ◽

Samanthula Kumara Swamy ◽

Alli Ramesh

Keyword(s):

Oral Bioavailability ◽

Oral Delivery ◽

Lipid Nanoparticles ◽

Delivery Systems ◽

Chemical Degradation ◽

Solid Lipid ◽

First Pass Metabolism ◽

First Pass ◽

Lipid Nanocarriers ◽

Pass Metabolism

Oral bioavailability of drugs is mainly limited due to the poor aqueous solubility, enhanced chemical degradation, reduced permeation and/or first pass metabolism. Various novel delivery systems are developed for improved oral bioavailability of these drugs such as modified orals, buccal, transdermal and osmotic delivery systems. Colloidal carrier systems such as nanoparticles, lipid nanoparticles, nanoemulsions, microspheres, liposomes, resealed erythrocytes and transfersomes were also developed to enhance the oral delivery. Among these, solid lipid nanocarriers (SLNs) also gain much attention on the enhancement of oral bioavailability. SLNs are submicron sized nanoparticles and composed of solid lipid, surfactants and cosurfactants. The enhanced oral bioavailability of poorly soluble drugs from SLNs might be due to the reduced particle size, bypassed presystemic metabolism, and enhanced gastric mucosa permeability. Vast literature is available for the advantages, limitations, preparation methods, evaluation parameters and application of SLNs in different routes. This review mainly focused on list of drugs developed as SLNs and considered as an alternative approach to enhance the oral bioavailability based on pharmacokinetic as well as pharmacodyanmic parameters was discussed. Keywords: Oral bioavailability, solubility, first-pass metabolism, solid lipid nanoparticles, pharmacokinetics, pharmacodynamics.

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Polymeric nanoparticles loaded naringin and naringenin: effect of solvent, characterization, photodegradation and stability studies

Drug Analytical Research ◽

10.22456/2527-2616.108783 ◽

2020 ◽

Vol 4 (2) ◽

pp. 64-71

Author(s):

Leticia Malgarim Cordenonsi ◽

Rafaela Martins Sponchiado ◽

Jardel Rodrigo Bandeira ◽

Roberto Chris Vianna Santos ◽

Renata Platchek Raffin ◽

...

Keyword(s):

Polymeric Nanoparticles ◽

Degradation Study ◽

Minimal Inhibitory Concentrations ◽

Transmission Electron ◽

First Pass Metabolism ◽

First Pass ◽

Uv C ◽

Inflammatory Action ◽

Pass Metabolism

Naringin (NAR) and naringenin (NGE) are flavonoids with important effects, such as antioxidant, nephroprotective and anti-inflammatory action. However, factors such as poor solubility and oral bioavailability, gastrointestinal instability and extensive first pass metabolism lead to limited deliverability. As far as we know, there are no papers describing the use of combination of NAR and NGE in nanoparticles. This paper describes the development and characterization of new nanoparticles containing NAR and NGE (NAR-NGE-NPs) which were prepared by nanoprecipitation using ethanol or mixture of solvents. Size distribution of NAR-NGE-NPs demonstrated a narrow distribution (121 nm), low polydispersity (< 0.1), and encapsulation efficiencies were greater than 80%. Infrared spectroscopy analyses confirmed the structure of NAR-NGE-NPs and in transmission electron microscopy, NAR-NGE-NPs presented a spherical and regular shape. A degradation study by UV-C, NAR-NGE-NPs improved photostability and conferred protection against NAR and NGE degradation. Minimal inhibitory concentrations of NAR and NGE were evaluated, however samples did not show antimicrobial activity. In this investigation, new NAR-NGE-NPs were successfully developed by a nanoprecipitation technique, using Endragit®L100 as polymer and ethanol as solvent.

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