Encapsulation of lipid-based formulations in porous carriers for controlled drug delivery

2021 ◽  
Vol 28 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Thao T.D. Tran
Keyword(s):  
Porous Materials ◽  
Controlled Drug Release ◽  
Water Soluble ◽  
Solid Dosage Forms ◽  
Pharmaceutical Ingredients ◽  
Solid Dosage ◽  
Water Soluble Drugs ◽  
Porous Carriers ◽  
Poorly Water Soluble ◽  
And Control

: Lipid-based formulations have recently been investigated as a promising approach to enhance the bioavailability of drugs, especially poorly water-soluble drugs. The encapsulation of lipid-based formulations in porous materials can result in a transformation of liquids or semisolid forms to solid dosage forms. Moreover, the specific structure of porous carriers could offer an enhanced ability to load and control active pharmaceutical ingredients. Although there have been prominent reports on lipid-based formulations and porous materials as promising technologies for controlled drug release, the overall methods of encapsulating lipid-based formulations need to be discussed for further formulation investigations. This review aims to present the key strategies used for producing porous carriers containing lipid-based formulations. We also discuss methods that enhance the encapsulation efficiency of loaded drugs within porous structures (instead of lipid-based formulations). Moreover, the critical factors that affect tablet formation are outlined. This overview of lipid-based formulations encapsulated within porous materials provides a summary of the technical methods used in the development of these formulations and their clinical translation.

scholarly journals LIQUISOLID COMPACT TECHNIQUES: A REVIEW

2018 ◽  
Vol 10 (4) ◽  
pp. 1
Author(s):  
Manisha Rokade ◽  
Pradnya Khandagale ◽  
Dipti Phadtare
Keyword(s):  
Drug Administration ◽  
Water Soluble ◽  
Oral Drug ◽  
Solid Dosage Forms ◽  
Coating Materials ◽  
Solid Dosage ◽  
Substantial Problem ◽  
Water Soluble Drugs ◽  
Insoluble Drugs ◽  
Routes Of Drug Administration

The poor dissolution rate of water-insoluble drugs is still a substantial problem confronting the pharmaceutical industry. There are several methods used to increase the solubility of drugs, of those liquid-solid compact technique is a new and promising addition towards such a novel aim, that the solubility of the insoluble drug moiety is increased by the aid of non-volatile solvents and hence increasing the dissolution and bioavailability. Oral drug administration has been one of the most convenient and widely accepted routes of delivery for most of the therapeutic agents. It is one of the most extensively used routes of drug administration because of its obvious advantages of ease of administration, improved patient compliance, and convenience. The enhancement of oral bioavailability of poorly water-soluble drugs remains one of the most challenging aspects of drug development. A more recent technique, “powdered solution technology” or “Liquisolid technology”, has been applied to prepare water-insoluble drugs into rapid-release solid dosage forms. The limited solubility of drugs is a challenging issue for the industry, during the development of the ideal solid dosage form unit. The technique is based upon the dissolving the insoluble drug in the nonvolatile solvent and admixture of drug loaded solutions with appropriate carrier and coating materials to convert into acceptably flowing and compressible powders.

scholarly journals Liquisolid systems and aspects influencing their research and development

2013 ◽  
Vol 63 (4) ◽  
pp. 447-465 ◽  
Author(s):  
Barbora Vraníková ◽  
Jan Gajdziok
Keyword(s):  
Surface Area ◽  
Absorption Capacity ◽  
Water Soluble ◽  
Production Costs ◽  
Load Factor ◽  
Solid Dosage Forms ◽  
Solid Dosage ◽  
Liquid Load ◽  
Simple Processing ◽  
Porous Carriers

Abstract Many modern drugs are poorly water soluble substances, which causes difficulties in the development of solid dosage forms with sufficient bioavailability. Preparation of liquisolid systems (LSS) is a novel technique for improving solubility, dissolution and bioavailability of such drugs. The basic principle of LSS preparation is conversion of the drug in liquid state into a free-flowing, compressible, dry powder through its absorption into suitable excipients - porous carriers (aluminometasilicates, microcrystalline cellulose), subsequently coated with material having high absorption capacity (silicon dioxide commonly known as colloidal silica). LSS exhibit advantages such as lower production costs compared to soft capsules, simple processing and enhanced drug release. The main benefit is higher bioavailability of the liquid drug, caused by a large surface area available for absorption. The article tries to clarify specific aspects connected with the formulation of LSS: properties of excipients (surface area, absorption capacity), variables related to the processing (solubility, liquid load factor) and dosage form evaluation.

scholarly journals Review on Polymer Based Nanoparticles for Increase the Bioavalibilty of Poorly Water Soluble Drug

2021 ◽  
pp. 56-74
Author(s):  
Karishma Mahajan ◽  
Nishant Thakur ◽  
. Simran
Keyword(s):  
Polymeric Nanoparticles ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Number Of Factors ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Review Study ◽  
And Control ◽  
Poorly Water Soluble Drug

In this review study about the polymeric nanoparticles and how polymer based nanoparticles increase bioavailability of less water soluble drugs. Polymeric nanoparticles have a matrix of biodegradable and biocompatible polymers of synthetic and natural origin. Polymer based nanoparticles are very useful for increase the solubility of the poor water-soluble drugs by decrease the particles size. Polymeric nanoparticles are very useful for targeting the drug to the specific site. Polymeric nanoparticles are also used to maintain and control the release of the drug. In present review study on the type of polymer used for the preparation of the polymer based nanoparticles. The choice of method depends on a number of factors, such as, particles size, area of application and characterization of polymeric nanoparticles.

scholarly journals Electrostatic Precipitation of Submicron Particles in a Molten Carrier

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 276
Author(s):  
Adrian Dobrowolski ◽  
Damian Pieloth ◽  
Helmut Wiggers ◽  
Markus Thommes
Keyword(s):  
Electrostatic Precipitator ◽  
Water Soluble ◽  
Submicron Particles ◽  
Dissolution Time ◽  
Poorly Water Soluble Drugs ◽  
Membrane Filters ◽  
Pharmaceutical Ingredients ◽  
Major Disadvantage ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Recently, submicron particles have been discussed as a means to increase the bioavailability of poorly water-soluble drugs. Separation of these small particles is done with both fibre and membrane filters, as well as electrostatic precipitators. A major disadvantage of an electrostatic precipitator (ESP) is the agglomerate formation on the precipitation electrode. These agglomerates frequently show low bioavailability, due to the decreased specific surface area and poor wettability. In this work, a new melt electrostatic precipitator was developed and tested to convert submicron particles into a solid dispersion in order to increase the bioavailability of active pharmaceutical ingredients. The submicron particles were generated by spray drying and transferred to the ESP, where the collection electrode is covered with a melt, which served as matrix after solidification. The newly developed melt electrostatic precipitator was able to collect isolated naproxen particles in a molten carrier. A solid naproxen xylitol dispersion was prepared, which showed a reduction of the dissolution time by 82%, and a release of 80% of the total drug, compared to the physical mixture.

Combined Use of Polymers and Porous Materials to Enhance Cinnarizine Dissolution

2019 ◽  
Vol 25 (4) ◽  
pp. 331-337
Author(s):  
Maryam Maghsoodi ◽  
Fatemeh Shahi
Keyword(s):  
Porous Materials ◽  
Dissolution Rate ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Water Soluble Drug ◽  
Dissolution Behaviour ◽  
Water Soluble Drugs ◽  
Poorly Soluble ◽  
Precipitation Inhibitor ◽  
Poorly Water Soluble

Background: Loading of poorly water-soluble drugs on the porous materials has attracted great interest as an effective approach for enhancement of dissolution rate of drugs. The Aerosil (Ae) with porous structure is expected to facilitate the dissolution of drugs which is generally associated with precipitation. Thus, the purpose of this investigation was thus to develop a formulation which combines a precipitation inhibitor and a poorly soluble drug loaded Ae. Methods: A poorly water-soluble drug, Cinnarizine (CNZ) was used as a model, and Eudragit L100 (Eu) was used as a precipitation inhibitor. Formulations were produced by solvent evaporation and characterized by FT-IR and differential scanning calorimetry (DSC). Dissolution experiments were carried out in phosphate buffer (pH 6.8) under non-sink conditions. Results: DSC thermograms revealed that no crystalline structure of CNZ was present in CNZ-loaded Ae formulations and no long-range order was arranged upon loading of CNZ into Ae. In dissolution test, the CNZ-loaded Ae physically blended with Eu achieved a remarkedly higher CNZ concentration over the plain CNZ and over the CNZ-Eu co-loaded Ae. The dissolution rate of CNZ from the CNZ-loaded Ae was enhanced with increasing Ae amount and the dissolution was maximum when the ratio of CNZ: Ae was 1:10 CNZ: Ae. In addition, the precipitation inhibition was increased when the amount of Eu was high. Conclusion: The results of this work revealed that the dissolution behaviour of CNZ-loaded Ae is enhanced by physically blending of Eu as a suitable precipitation inhibitor.

scholarly journals Enhancement of solubility of poorly soluble drugs by solid dispersion: An Overview

2017 ◽  
Vol 5 (04) ◽  
pp. 17-23
Author(s):  
Katta Manogna ◽  
P. Nagaveni ◽  
K. Thyagaraju
Keyword(s):  
Solid Dispersion ◽  
Oral Absorption ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Drug Solubility ◽  
Solid Dosage Forms ◽  
Preparation Methods ◽  
Solid Dosage ◽  
Poorly Soluble ◽  
Poorly Water Soluble

Most of the newly invented chemical drug moieties are poorly water soluble. According to BCS classification, class II and IV drugs are considered as poorly water soluble. So enhancement of oral absorption and bioavailability of solid dosage forms remains a challenge to formulation scientists due to their solubility criteria. Therefore many techniques are being explored to enhance the solubility of poor soluble drugs. Solid dispersion is one of the most important method for enhance the solubility (dissolution rate) and hence oral bioavailability of poorly soluble drugs. In solid dispersion the particle size of drug is reduced or a crystalline pure drug is converted into amorphous form and hence the solubility is increased. Polymer incorporating in solid dispersion technology is usually hydrophilic in nature and also showing compatibility with the drug to enhance the drug solubility. This review mainly discus about solid dispersion, preparation methods, and finally characterization.

scholarly journals Understanding the Role of Sodium Lauryl Sulfate on the Biorelevant Solubility of a Combination of Poorly Water-Soluble Drugs Using High Throughput Experimentation and Mechanistic Absorption Modeling

2019 ◽  
Vol 22 ◽  
pp. 221-246 ◽  
Author(s):  
Matthew Nathan Bahr ◽  
Dimple Modi ◽  
Sarsvatkumar Patel ◽  
Gossett Campbell ◽  
Gregory Stockdale
Keyword(s):  
High Throughput ◽  
Dosage Form ◽  
Water Soluble ◽  
Lauryl Sulfate ◽  
Solid Dosage Form ◽  
Solid Dosage ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Free Energy Of Micellization

This study investigates the influence of surfactant sodium lauryl sulfate (SLS) on the solubility of poorly-water soluble drug substances, model Compound X and Compound Y, used in a fixed dose combination oral solid dosage form. To determine the impact of SLS concentration on the solubility of compounds X and Y, we experimentally determined the critical micelle concentration (CMC) of SLS in water, simulated gastric fluid (SGF), and fed state simulated intestinal fluid (FeSSIF) in the presence of Compound X and Compound Y using UV/Visible spectrophotometry at 25°C. The aggregation of SLS was characterized by calculating the standard Gibbs free energy of micellization in all the media investigated.  To enhance the understanding of SLS aggregation, high throughput experiments and in-vivo mechanistic modelling were used to determine the effect of increasing levels of SLS on the solubility of compounds X and Y as both single agent and combination products to be formulated into a suitable oral solid dosage form. Micellar formation of SLS is a spontaneous process as shown by the negative values of the standard free energy of micellization. The CMC of SLS in the various media investigated in the presence of compounds X and Y decreases in the following order: water> FeSSIF> SGF. However, the aggregation of SLS in the various media is overall more spontaneous in the following order: SGF>FeSSIF>water. Using high throughput experimentation and in-vivo mechanistic modelling, it was determined that a combination oral solid product of compounds X and Y will have optimum solubility and in-vivo absorption if 2 mg of SLS was used in the oral solid dosage form.  The results obtained from this study will help broaden the understanding of the micellization process involving SLS and poorly-water soluble drugs used in combination oral solid dosage forms.

Degradation Mechanisms for Water-Soluble Drugs in Solid Dosage Forms

1969 ◽  
Vol 58 (5) ◽  
pp. 549-553 ◽  
Author(s):  
J.Thurø Carstensen ◽  
Modest Osadca ◽  
S.H. Rubin
Keyword(s):  
Dosage Forms ◽  
Water Soluble ◽  
Degradation Mechanisms ◽  
Solid Dosage Forms ◽  
Solid Dosage ◽  
Water Soluble Drugs
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