Role of polymer/polymer and polymer/drug specific interactions in drug delivery systems

2019 ◽  
Vol 39 (6) ◽  
pp. 534-544
Author(s):  
Farid Ouazib ◽  
Naima Bouslah Mokhnachi ◽  
Nabila Haddadine ◽  
Regis Barille

Abstract Drug delivery systems based upon the blending of Arabic gum and poly(N-vinylpyrrolidone) (AG/PVP) were prepared for the controlled release of acebutolol (Acb) hydrochloride. The prepared blends containing Acb were characterized using different techniques. The presence of physical interactions between the drug and polymer matrices was observed with Fourier-transform infrared spectroscopy. These interactions resulted in the transition of the drug from a crystalline to an amorphous state into the polymeric matrices, as demonstrated by differential scanning calorimetry and X-ray diffraction analysis. The thermogravimetric analysis study confirmed the presence of these interactions, which had a stabilizing effect on the drug against both thermal degradation and crystallinity. The in vitro release of Acb from the AG/PVP polymer system was investigated. Each drug-loaded system was used in a tablet formulation. Moreover, an in vitro dissolution study was carried out in three different dissolution media, and comparison of the dissolution profiles of the different dosage forms revealed that the polymer blend matrix had a better release-retarding efficiency. To better understand the release mechanism, the dissolution data were fitted to various release kinetic models.

Materials ◽  
2020 ◽  
Vol 13 (2) ◽  
pp. 329 ◽  
Author(s):  
Daria Lovskaya ◽  
Natalia Menshutina

The present work focuses on the preparation of alginate-based aerogels in the form of particles for their further study as potential drug delivery systems (solid dosage forms). The dripping method was used to prepare certain gel particles, and supercritical drying was used to obtain final alginate-based aerogel particles. Three model active substances (ketoprofen, nimesulide, loratadine) were impregnated into the obtained aerogels using the supercritical adsorption process. Using the method of X-ray analysis, it was shown that the in the obtained drug-loaded aerogels the corresponding active substances are in an amorphous state, and the stability of this state after six months of storage is confirmed. In vitro dissolution tests for obtained drug-loaded aerogels was performed. For each sample, an appropriate dissolution medium (with certain pH) was determined. In vitro investigations showed the increasing of the release rate for all model active substances. Time was required to release and dissolve 50% of the active drug from drug-loaded aerogels (T1/2), reduced in comparison with pure active drugs in crystalline form. Obtained results provide insight into the application of alginate-based aerogel particles as a drug delivery system to improve pharmacokinetic properties of certain active drugs.


2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Urve Paaver ◽  
Ingrid Tamm ◽  
Ivo Laidmäe ◽  
Andres Lust ◽  
Kalle Kirsimäe ◽  
...  

Electrospinning is an effective method in preparing polymeric nanofibrous drug delivery systems (DDSs) for topical wound healing and skin burn therapy applications. The aim of the present study was to investigate a new synthetic graft copolymer (Soluplus) as a hydrophilic carrier polymer in electrospinning of nanofibrous DDSs. Soluplus (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCL-PVAc-PEG)) was applied in the nonwoven nanomats loaded with piroxicam (PRX) as a poorly water-soluble drug. Raman spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and scanning electron microscopy (SEM) were used in the physical characterization of nanofibrous DDSs. According to the SEM results, the drug-loaded PCL-PVAc-PEG nanofibers were circular in cross-section with an average diameter ranging from 500 nm up to 2 µm. Electrospinning stabilized the amorphous state of PRX. In addition, consistent and sustained-release profile was achieved with the present nanofibrous DDSs at the physiologically relevant temperature and pH applicable in wound healing therapy. In conclusion, electrospinning can be used to prepare nanofibrous DDSs of PCL-PVAc-PEG graft copolymer (Soluplus) and to stabilize the amorphous state of a poorly water-soluble PRX. The use of this synthetic graft copolymer can open new options to formulate nanofibrous DDSs for wound healing.


2015 ◽  
Vol 65 (1) ◽  
pp. 29-42 ◽  
Author(s):  
Gamal Shazly ◽  
Kazi Mohsin

Abstract Solidification of lipid formulations using adsorbents is a recent technique attracting great interest due to its favourable properties including flexibility in dose division, reduction of intra-subject and inter-subject variability, improvement in efficacy/safety profile and enhancement of physical/ chemical stability. The current study aims to convert liquid self-emulsifying/nanoemulsifying drug delivery systems (SEDDS/SNEDDS) into solid SEDDS/SNEDDS and to assess how adsorption of the drug onto an inorganic high surface area material, NeusilinR grade US2 (NUS2), affects its in vitro dissolution performance. Lipid formulation classification systems (LFCS) Type III formulations were designed for the model anti-cholesterol drug fenofibrate. NUS2 was used to solidify the SEDDS/SNEDDS. Particle size and SEM analyses of solid SEDDS/SNEDDS powder were carried out to investigate the adsorption efficiency. In vitro dissolution studies were conducted to compare the developed formulations with the marketed product. The results of characterization studies showed that the use of 50 % (m/m) adsorbent resulted in superior flowability and kept the drug stable is amorphous state. Dissolution studies allow the conclusion that the formulation containing a surfactant of higher water solubility (particularly, Type IIIB SNEDDS) has comparably faster and higher release profiles than Type IIIA (SEDDS) and marketed product


2019 ◽  
Vol 26 (14) ◽  
pp. 2502-2513 ◽  
Author(s):  
Md. Iqbal Hassan Khan ◽  
Xingye An ◽  
Lei Dai ◽  
Hailong Li ◽  
Avik Khan ◽  
...  

The development of innovative drug delivery systems, versatile to different drug characteristics with better effectiveness and safety, has always been in high demand. Chitosan, an aminopolysaccharide, derived from natural chitin biomass, has received much attention as one of the emerging pharmaceutical excipients and drug delivery entities. Chitosan and its derivatives can be used for direct compression tablets, as disintegrant for controlled release or for improving dissolution. Chitosan has been reported for use in drug delivery system to produce drugs with enhanced muco-adhesiveness, permeation, absorption and bioavailability. Due to filmogenic and ionic properties of chitosan and its derivative(s), drug release mechanism using microsphere technology in hydrogel formulation is particularly relevant to pharmaceutical product development. This review highlights the suitability and future of chitosan in drug delivery with special attention to drug loading and release from chitosan based hydrogels. Extensive studies on the favorable non-toxicity, biocompatibility, biodegradability, solubility and molecular weight variation have made this polymer an attractive candidate for developing novel drug delivery systems including various advanced therapeutic applications such as gene delivery, DNA based drugs, organ specific drug carrier, cancer drug carrier, etc.


2015 ◽  
Vol 51 (2) ◽  
pp. 255-263
Author(s):  
Rupali Nanasaheb Kadam ◽  
Raosaheb Sopanrao Shendge ◽  
Vishal Vijay Pande

<p>The use of nanotechnology based on the development and fabrication of nanostructures is one approach that has been employed to overcome the challenges involved with conventional drug delivery systems. Formulating Nanoplex is the new trend in nanotechnology. A nanoplex is a complex formed by a drug nanoparticle with an oppositely charged polyelectrolyte. Both cationic and anionic drugs form complexes with oppositely charged polyelectrolytes. Compared with other nanostructures, the yield of Nanoplex is greater and the complexation efficiency is better. Nanoplex are also easier to prepare. Nanoplex formulation is characterized through the production yield, complexation efficiency, drug loading, particle size and zeta potential using scanning electron microscopy, differential scanning calorimetry, X-ray diffraction and dialysis studies. Nanoplex have wide-ranging applications in different fields such as cancer therapy, gene drug delivery, drug delivery to the brain and protein and peptide drug delivery.</p>


Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 861
Author(s):  
Jacopo Cardellini ◽  
Arianna Balestri ◽  
Costanza Montis ◽  
Debora Berti

In the past decade(s), fluorescence microscopy and laser scanning confocal microscopy (LSCM) have been widely employed to investigate biological and biomimetic systems for pharmaceutical applications, to determine the localization of drugs in tissues or entire organisms or the extent of their cellular uptake (in vitro). However, the diffraction limit of light, which limits the resolution to hundreds of nanometers, has for long time restricted the extent and quality of information and insight achievable through these techniques. The advent of super-resolution microscopic techniques, recognized with the 2014 Nobel prize in Chemistry, revolutionized the field thanks to the possibility to achieve nanometric resolution, i.e., the typical scale length of chemical and biological phenomena. Since then, fluorescence microscopy-related techniques have acquired renewed interest for the scientific community, both from the perspective of instrument/techniques development and from the perspective of the advanced scientific applications. In this contribution we will review the application of these techniques to the field of drug delivery, discussing how the latest advancements of static and dynamic methodologies have tremendously expanded the experimental opportunities for the characterization of drug delivery systems and for the understanding of their behaviour in biologically relevant environments.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1108
Author(s):  
Oana Craciunescu ◽  
Madalina Icriverzi ◽  
Paula Ecaterina Florian ◽  
Anca Roseanu ◽  
Mihaela Trif

Osteoarthritis (OA) is a degenerative joint disease. An objective of the nanomedicine and drug delivery systems field is to design suitable pharmaceutical nanocarriers with controllable properties for drug delivery and site-specific targeting, in order to achieve greater efficacy and minimal toxicity, compared to the conventional drugs. The aim of this review is to present recent data on natural bioactive compounds with anti-inflammatory properties and efficacy in the treatment of OA, their formulation in lipid nanostructured carriers, mainly liposomes, as controlled release systems and the possibility to be intra-articularly (IA) administered. The literature regarding glycosaminoglycans, proteins, polyphenols and their ability to modify the cell response and mechanisms of action in different models of inflammation are reviewed. The advantages and limits of using lipid nanoformulations as drug delivery systems in OA treatment and the suitable route of administration are also discussed. Liposomes containing glycosaminoglycans presented good biocompatibility, lack of immune system activation, targeted delivery of bioactive compounds to the site of action, protection and efficiency of the encapsulated material, and prolonged duration of action, being highly recommended as controlled delivery systems in OA therapy through IA administration. Lipid nanoformulations of polyphenols were tested both in vivo and in vitro models that mimic OA conditions after IA or other routes of administration, recommending their clinical application.


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