scholarly journals Low-Surfactant Microemulsions for Enhanced Topical Delivery of Poorly Soluble Drugs

2011 ◽  
Vol 14 (3) ◽  
pp. 315 ◽  
Author(s):  
Alireza Shalviri ◽  
Avinash C Sharma ◽  
Dipak Patel ◽  
Amyn Sayani
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Colloidal Silica ◽  
Topical Delivery ◽  
Silica Gels ◽  
Poorly Soluble Drugs ◽  
Release Rates ◽  
Significant Difference ◽  
Poorly Soluble ◽  
Model Drug

Purpose: To develop and characterize low-surfactant microemulsion (ME) gels to enhance topical delivery of poorly soluble drugs. Method: Five low surfactant ME formulations were manufactured following the construction of pseudo-ternary phase diagrams. The MEs were screened for their ability to dissolve a poorly soluble new chemical entity (Model Drug X). Various viscosity imparting agents like Carbopol 934, Colloidal Silica, HPMC K100M, Lubrajel NP, and Xanthan Gum were evaluated for the manufacture of these ME gels. Each ME gel was then further evaluated for physical stability, including assessing rheological profiles. In vitro release profiles were also determined and compared to a conventional ointment. Results: Three of the five low surfactant MEs developed (ME1, ME4 and ME5) were capable of dissolving Model Drug X up to 14 fold higher than the conventional ointment formulation. ME1 and ME4 gels comprising Xanthan gum or Carbopol 934 were physically stable, while ME5 gel was stable only with Colloidal Silica. The ME5 gel with Colloidal Silica showed an irreversible increase in its elastic modulus when exposed to high temperature, indicating that the formulation would be less suitable for commercial use. The Xanthan Gum and Colloidal Silica gels yielded significantly higher release rates (8 - 10 fold) compared to a conventional ointment and formulations containing Carbopol 934. The significant difference in drug release rates between Xanthan Gum and Carbopol 934 indicated that choice of viscosity imparting agent played an important role in governing drug release from ME gels. Conclusion: ME gels were developed with low surfactant concentrations and improved formulation characteristics, which increased the solubility and subsequent release of a poorly soluble drug. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

scholarly journals Effect of compression pressure on mechanical and release properties of tramadol matrix tablets

2015 ◽  
Vol 28 (2) ◽  
pp. 120-125 ◽  
Author(s):  
Olutayo A. Adeleye ◽  
Mbang N. Femi-Oyewo ◽  
Michael A. Odeniyi
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
The Body ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Sodium Carboxymethylcellulose ◽  
Compression Pressure ◽  
Significant Difference ◽  
Tablet Manufacturing ◽  
Tablet Hardness

Abstract Drug delivery to the proper site of action in the body is greatly influenced by the excipients used and some processing variables such as changes in compression force. The aim of this investigation was to study the influence of changes in compression forces during tablet manufacturing on the mechanical and release properties of Tramadol matrix tablet. Hardness and friability were used as assessment parameters for mechanical properties while release properties were analysed using dissolution test. Data were analysed using One-way ANOVA at p < 0.05. Tablet hardness and friability were typically compression pressure-dependent with a significant difference in tablet hardness and friability with increase in compression pressure (p < 0.001). Drug release was best expressed by Korsmeyer-Peppas equation as the plots showed high linearity (r2) of 0.998 and 0.988 for formulations containing Xanthan gum and Sodium carboxymethylcellulose, respectively. Drug release from formulations containing Xanthan gum was mainly by diffusion while a combination of diffusion and chain relaxation was the mechanism of drug release from formulation containing Sodium Carboxymethylcellulose. The release properties of tramadol matrix tablet were not significantly influenced by compression pressure but rather by the polymer and the material properties of the drug.

Preparation and Release Profiles of a Solid Oleoylchitosan Coated Poly(lactic-co-glycolic acid) Nanoparticles

2014 ◽  
Vol 936 ◽  
pp. 717-722
Author(s):  
Yan Yan Li ◽  
Feng Song Liu
Keyword(s):  
Drug Release ◽  
Glycolic Acid ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Release Behavior ◽  
Release Rates ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency ◽  
Model Drug

A solid oleoylchitosan (OCS) coated Poly (lactic-co-glycolic acid) (PLGA) nanoparticles (OCS-coated PLGA NPs) were prepared using the emulsification–evaporation method. The nanoparticles in suspension (TEM) and solid state (SEM) were spherical and very regular and compact. The effects of OCS concentration, PLGA concentration, drug concentration, and release media on drug entrapment efficiency and in vitro drug release behavior were investigated for the release properties using rifampicin (RFP) as a model drug. Both the increase of PLGA concentration and the increase of OCS concentration could decrease the drug release rates. The RFP release rates decreased as the RFP concentration increased. The RFP release rate was sensitive to the pH of the release media.

scholarly journals A Novel Solid Nanocrystals Self-Stabilized Pickering Emulsion Prepared by Spray-Drying with Hydroxypropyl-β-cyclodextrin as Carriers

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1809
Author(s):  
Jifen Zhang ◽  
Yanhua Wang ◽  
Jirui Wang ◽  
Tao Yi
Keyword(s):  
Spray Drying ◽  
Laser Scanning ◽  
Pickering Emulsion ◽  
Water Soluble ◽  
Laser Scanning Microscopy ◽  
Confocal Laser ◽  
Poorly Soluble Drugs ◽  
Significant Difference ◽  
Poorly Soluble

A drug nanocrystals self-stabilized Pickering emulsion (NSSPE) with a unique composition and microstructure has been proven to significantly increase the bioavailability of poorly soluble drugs. This study aimed to develop a new solid NSSPE of puerarin preserving the original microstructure of NSSPE by spray-drying. A series of water-soluble solid carriers were compared and then Box-Behnken design was used to optimize the parameters of spray-drying. The drug release and stability of the optimized solid NSSPE in vitro were also investigated. The results showed that hydroxypropyl-β-cyclodextrin (HP-β-CD), rather than solid carriers commonly used in solidification of traditional Pickering emulsions, was suitable for the solid NSSPE to retain the original appearance and size of emulsion droplets after reconstitution. The amount of HP-β-CD had more influences on the solid NSSPE than the feed rate and the inlet air temperature. Fluorescence microscopy, confocal laser scanning microscopy and scanning electron microscopy showed that the reconstituted emulsion of the solid NSSPE prepared with HP-β-CD had the same core-shell structure with a core of oil and a shell of puerarin nanocrystals as the liquid NSSPE. The particle size of puerarin nanocrystal sand interfacial adsorption rate also did not change significantly. The cumulative amount of released puerarin from the solid NSSPE had no significant difference compared with the liquid NSSPE, which were both significantly higher than that of puerarin crude material. The solid NSSPE was stable for 3 months under the accelerated condition of 75% relative humidity and 40 °C. Thus, it is possible todevelop the solid NSSPE preserving the unique microstructure and the superior properties in vitro of the liquid NSSPE for poorly soluble drugs.

scholarly journals Design and evaluation of lornoxicam bilayered tablets for biphasic release

2012 ◽  
Vol 48 (4) ◽  
pp. 609-619
Author(s):  
Songa Ambedkar Sunil ◽  
Meka Venkata Srikanth ◽  
Nali Sreenivasa Rao ◽  
Sakamuri Balaji ◽  
Kolapalli Venkata Ramana Murthy
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Hydroxypropyl Methylcellulose ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Release Kinetic ◽  
Burst Release ◽  
Significant Difference ◽  
Biphasic Release

The objective of the present investigation was to develop bilayered tablets of lornoxicam to achieve biphasic release pattern. A bilayered tablet, consisting of an immediate and controlled release layer, was prepared by direct compression technique. The controlled release effect was achieved by using various hydrophilic natural, semi synthetic and synthetic controlled release polymers such as xanthan gum, hydroxypropyl methylcellulose (HPMC) and polyethylene oxide (PEO) to modulate the release of the drug. The in vitro drug release profiles showed the biphasic release behavior in which the immediate release (IR) layer containing the lornoxicam was released within 15 minutes, whereas the controlled release (CR) layer controlled the drug release for up to 24 h. All the bilayered tablets formulated have followed the zero order release with non-Fickian diffusion controlled release mechanism after the initial burst release. FTIR studies revealed that there was no interaction between the drug and polymers used in the study. Statistical analysis (ANOVA) showed no significant difference in the cumulative amount of drug release after 15 min, but significant difference (p < 0.05) in the amount of drug released after 24 h from optimized formulations was observed. Based on the release kinetic parameters obtained, it can be concluded that xanthan gum polymer was suitable for providing a biphasic release of lornoxicam.

Vitamin B12 Release from P(HEMA-co-THFMA) in Water and SBF: A Model Drug Release Study

2005 ◽  
Vol 58 (6) ◽  
pp. 451 ◽  
Author(s):  
Mohammad A. Chowdhury ◽  
David J. T. Hill ◽  
Andrew K. Whittaker
Keyword(s):  
Drug Release ◽  
Vitamin B12 ◽  
Diffusion Mechanism ◽  
Fickian Diffusion ◽  
Copolymer Composition ◽  
Release Rates ◽  
Drug Release Study ◽  
Release Study ◽  
Model Drug ◽  
Sbf Solution

A model drug release study on the ingress of water and Kokubo simulated body fluid (SBF) into poly(2-hydroxyethyl methacrylate) (P(HEMA)) and its copolymers with tetrahydrofurfuryl methacrylate (THFMA) loaded with vitamin B12 was undertaken over the temperature range 298–318 K. The polymers were studied as cylinders and were loaded with either 5 or 10 wt-% of the drug. The drug release from the polymers was found to follow a Fickian diffusion mechanism in the early stages of the drug release, with higher normalized release rates at higher temperatures and higher drug loadings. The normalized release rates were also found to be higher for the SBF solution than for water. The copolymer composition was found to have a significant effect on the rate of release of the drug, with the rate falling rapidly between HEMA mole fractions of 1.0 and 0.8, but for lower mole fractions of HEMA the normalized release rate decreased more slowly. This behaviour followed the trend found for the changes in the equilibrium penetrant contents for the copolymers.

scholarly journals 3D-Printed Mesoporous Carrier System for Delivery of Poorly Soluble Drugs

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1096
Author(s):  
Christos S. Katsiotis ◽  
Michelle Åhlén ◽  
Maria Strømme ◽  
Ken Welch
Keyword(s):  
Drug Release ◽  
Mesoporous Materials ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Great Promise ◽  
Poorly Soluble Drugs ◽  
Drug Concentrations ◽  
Poorly Soluble ◽  
3D Printed ◽  
Oral Dosage Forms

Fused deposition modelling (FDM) is the most extensively employed 3D-printing technique used in pharmaceutical applications, and offers fast and facile formulation development of personalized dosage forms. In the present study, mesoporous materials were incorporated into a thermoplastic filament produced via hot-melt extrusion and used to produce oral dosage forms via FDM. Mesoporous materials are known to be highly effective for the amorphization and stabilization of poorly soluble drugs, and were therefore studied in order to determine their ability to enhance the drug-release properties in 3D-printed tablets. Celecoxib was selected as the model poorly soluble drug, and was loaded into mesoporous silica (MCM-41) or mesoporous magnesium carbonate. In vitro drug release tests showed that the printed tablets produced up to 3.6 and 1.5 times higher drug concentrations, and up to 4.4 and 1.9 times higher release percentages, compared to the crystalline drug or the corresponding plain drug-loaded mesoporous materials, respectively. This novel approach utilizing drug-loaded mesoporous materials in a printed tablet via FDM shows great promise in achieving personalized oral dosage forms for poorly soluble drugs.

scholarly journals Nanoporous Silica Entrapped Lipid-Drug Complexes for the Solubilization and Absorption Enhancement of Poorly Soluble Drugs

Pharmaceutics ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 63
Author(s):  
Hey-Won Shin ◽  
Joo-Eun Kim ◽  
Young-Joon Park
Keyword(s):  
Ternary Phase Diagram ◽  
Absorption Enhancement ◽  
Nanoporous Silica ◽  
Pharmacokinetic Studies ◽  
Poorly Soluble Drugs ◽  
Scanning Calorimetry ◽  
Significant Difference ◽  
High Dissolution Rate ◽  
Polyethylene Glycol 1000 ◽  
Poorly Soluble

This study aims to examine the contribution of nanoporous silica entrapped lipid-drug complexes (NSCs) in improving the solubility and bioavailability of dutasteride (DUT). An NSC was loaded with DUT (dissolved in lipids) and dispersed at a nanoscale level using an entrapment technique. NSC microemulsion formation was confirmed using a ternary phase diagram, while the presence of DUT and lipid entrapment in NSC was confirmed using scanning electron microscopy. Differential scanning calorimetry and X-ray diffraction revealed the amorphous properties of NSC. The prepared all NSC had excellent flowability and enhanced DUT solubility but showed no significant difference in drug content homogeneity. An increase in the lipid content of NSC led to an increase in the DUT solubility. Further the NSC were formulated as tablets using D-α tocopheryl polyethylene glycol 1000 succinate, glyceryl caprylate/caprate, and Neusilin®. The NSC tablets showed a high dissolution rate of 99.6% at 30 min. Furthermore, NSC stored for 4 weeks at 60 °C was stable during dissolution testing. Pharmacokinetic studies performed in beagle dogs revealed enhanced DUT bioavailability when administered as NSC tablets. NSC can be used as a platform to develop methods to overcome the technical and commercial limitations of lipid-based preparations of poorly soluble drugs.

scholarly journals Novel Nanoparticle Biomaterial of Alginate/Chitosan Loading Simultaneously Lovastatin and Ginsenoside RB1: Characteristics, Morphology, and Drug Release Study

2021 ◽  
Vol 2021 ◽  
pp. 1-14
Author(s):  
Quan Vo-An ◽  
Thuy Chinh Nguyen ◽  
Quang Tung Nguyen ◽  
Quoc Trung Vu ◽  
Cong Doanh Truong ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Tripolyphosphate ◽  
Poorly Soluble Drugs ◽  
Drug Solubility ◽  
Ginsenoside Rb1 ◽  
Scanning Calorimetry ◽  
Release Process ◽  
Polymeric Particles ◽  
Poorly Soluble ◽  
Initial Content

Recently, plenty of interesting studies on improvement of bioavailability for poorly soluble drugs were implemented with different approaches such as using of combined biopolymers as a delivery system that allowed to enhancing drug solubility and bioavailability. In this work, alginate and chitosan were blended together in the form of polymeric particles, loaded with both lovastatin and ginsenoside Rb1 to producing the four-component nanoparticles by ionic gelation method. CaCl2 and sodium tripolyphosphate were used as gelation agent and cross-linking agent, respectively. The characteristics of obtained nanoparticles were studied by means of infrared spectra (IR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and dynamic light scattering (DLS). In combination, ginsenoside Rb1 and lovastatin both interacted with each other to improve the drug release ability of the polymer particles. The change of initial content of drugs in the nanoparticles has a negligible effect on the functional groups in the structure of the nanoparticles but has a significant impact on drug release process of both lovastatin and ginsenoside Rb1 from the nanoparticles in selective simulated body fluids. In addition, the synergistic interaction of lovastatin and ginsenoside Rb1 could be also observed through the modification of relative crystal degree and drug release efficiency.

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