Understanding the Thermodynamic Mechanisms Leading to the Binding of Albumin to Lipid Nanocapsules.

Lipid nanocapsules (LNCs) are drug delivery platforms designed for different administration routes including intravenous delivery. Nanocarrier binding with plasma proteins such as albumin is an important factor that influences the pharmacokinetics of the drug and the drug delivery system. The aim of this paper was to characterize LNCs with different surface compositions and hydrophobicities to study their interactions with albumin: binary LNCs [oil-glyceryl trioctanoate (TG) and PEGylated surfactant macrogol 15-hydroxystearate (MHS)] and ternary LNCs (TG, MHS, and Span 80). Span was found to stabilize and decrease the LNC size. The formation of a stable LNC/albumin complex in the ground state was demonstrated. Thermodynamic parameters indicated that complex formation was exothermic and spontaneous, and the interactions involved van der Waals forces and hydrogen bond formation. Ternary LNCs showed higher affinity for albumin than did binary LNCs (affinity constant 10-fold higher). This study is the first report on the thermodynamic mechanisms that lead to the formation of a complex between albumin and organic nanoparticles with different surface architectures.

Polymer nanocomposites enhance S-nitrosoglutathione intestinal absorption and promote the formation of releasable nitric oxide stores in rat aorta.

Alginate/chitosan nanocomposite particles (GSNO-acNCPs), i.e. S-nitrosoglutathione (GSNO) loaded polymeric nanoparticles incorporated into an alginate and chitosan matrix, were developed to increase the effective GSNO loading capacity, a nitric oxide (NO) donor, and to sustain its release from the intestine following oral administration. Compared with free GSNO and GSNO loaded nanoparticles, GSNO-acNCPs promoted 2.7-fold GSNO permeation through a model of intestinal barrier (Caco-2 cells). After oral administration to Wistar rats, GSNO-acNCPs promoted NO storage into the aorta during at least 17h, as highlighted by (i) a long-lasting hyporeactivity to phenylephrine (decrease in maximum vasoconstrictive effect of aortic rings) and (ii) N-acetylcysteine (a thiol which can displace NO from tissues)-induced vasodilation of aorxxtic rings preconstricted with phenylephrine. In conclusion, GSNO-acNCPs enhance GSNO intestinal absorption and promote the formation of releasable NO stores into the rat aorta. GSNO-acNCPs are promising carriers for chronic oral application devoted to the treatment of cardiovascular diseases.

Albumin as a carrier for NO delivery: preparation, physicochemical characterization, and interaction with gold nanoparticles.

BACKGROUND: Nitric oxide (NO) is a gaseous transmitter playing numerous physiological roles and characterized by a short half-life. Its binding to endogenous thiols increases its stability, facilitating its storage and transport. The purpose of this study was to investigate the nitrosated serum albumin (SA-SNO) and to provide a reference for its easy preparation for further use in in vitro studies. METHODS: Serum albumin (SA) was S-nitrosated by reacting with (i) NaNO2 in acidic medium; (ii) different low-molecular weight S-nitrosothiols (RSNO) (S-nitrosocysteine (CysNO), S-nitrosoglutathione (GSNO), and S,S'-dinitrosobucillamine (Buc(NO)2)); and (iii) diethylamine NONOate (DEA/NO). SA-SNO was purified by size exclusion chromatography and the S-nitrosation site and the rate were studied by mass spectrometry and Griess-Saville assay, respectively. Then, SA-SNO was characterized by spectrofluorimetry, dynamic light scattering, and circular dichroism. Finally, SA-SNO reactivity with citrate stabilized gold nanoparticles (AuNP-citrate) was investigated via determination of NO release. RESULTS: S-nitrosation rates of SA were 90.1 ± 3.3, 76.8 ± 2.7, 80.3 ± 3.2, 84.8 ± 5.0, and 15.4 ± 1.9% (n = 5), when SA was reacted with acidified NaNO2, CysNO, GSNO, Buc(NO)2, and DEA/NO, respectively. The physicochemical characterization indicated that the resulting product corresponded to a mono-S-nitrosothiol (on cysteine-34), and the conformational construction remained unchanged. Stability studies showed that the NO content was preserved over 1 week. AuNP-citrate reacted with SA-SNO with increase of its hydrodynamic diameter but preservation of SNO bond. CONCLUSIONS: SA-SNO prepared and stored under the reported conditions affords a well-defined reference suitable for in vitro studies.

Doxorubicin-loaded glycyrrhetinic acid modified recombinant human serum albumin nanoparticles for targeting liver tumor chemotherapy.

Due to overexpression of glycyrrhetinic acid (GA) receptor in liver cancer cells, glycyrrhetinic acid modified recombinant human serum albumin (rHSA) nanoparticles for targeting liver tumor cells may result in increased therapeutic efficacy and decreased adverse effects of cancer therapy. In this study, doxorubicin (DOX) loaded and glycyrrhetinic acid modified recombinant human serum albumin nanoparticles (DOX/GA-rHSA NPs) were prepared for targeting therapy for liver cancer. GA was covalently coupled to recombinant human serum albumin nanoparticles, which could efficiently deliver DOX into liver cancer cells. The resultant GA-rHSA NPs exhibited uniform spherical shape and high stability in plasma with fixed negative charge (∼-25 mV) and a size about 170 nm. DOX was loaded into GA-rHSA NPs with a maximal encapsulation efficiency of 75.8%. Moreover, the targeted NPs (DOX/GA-rHSA NPs) showed increased cytotoxic activity in liver tumor cells compared to the nontargeted NPs (DOX/rHSA NPs, DOX loaded recombinant human serum albumin nanoparticles without GA conjugating). The targeted NPs exhibited higher cellular uptake in a GA receptor-positive liver cancer cell line than nontargeted NPs as measured by both flow cytometry and confocal laser scanning microscopy. Biodistribution experiments showed that DOX/GA-rHSA NPs exhibited a much higher level of tumor accumulation than nontargeted NPs at 1 h after injection in hepatoma-bearing Balb/c mice. Therefore, the DOX/GA-rHSA NPs could be considered as an efficient nanoplatform for targeting drug delivery system for liver cancer.

[Counterfeit and Falsified Drugs: an Overview]. / Trafic de faux médicaments : panorama 2014.

If the traffic of fake medicines may represent an economic threat for the pharmaceutical industry, it can also be responsible of safety concerns for patients. Despite fake drugs represent a real threat for public health, the intended punishments are until now only based on intellectual property rights. Estimated to generate more than 55 billion euros per year, the traffic of falsified drugs varies from a country to another one. Indeed, the proportion of falsified drugs ranges from 1% in industrialized countries with a regulated and controlled distribution system to 60% of medicines in some developing countries. Currently, the measures developed to limit this traffic concern five main areas: legislation / regulation, cooperation, enforcement, technology and communication. Communication actions should be performed to inform health professionals as the populations about the risks of using drugs purchased outside the legal drug market.

Food-inspired innovations to improve the stability of active pharmaceutical ingredients.

Food-processing and pharmaceutical industries share a lot of stability issues against the same physical, chemical, and microbiological phenomena. They also share some solutions to improve the stability as the use of preservatives and packaging. Ecological concerns lead to the development of tremendous innovations in food. Some of these innovations could also be beneficial in the pharmaceutical domain. The objective of this review is to evaluate the potential application of these findings in the pharmaceutical field and the main limits in terms of toxicity, environmental, economic and regulatory issues. The principal factors influencing the shelf-life were highlighted through the description of the stability studies usually performed in the pharmaceutical industry (according to European guidelines). To counter those factors, different solutions are currently available as preservatives and specific packaging. They were described and debated with an overview of recent food innovations in each field. The limits of the current solutions in the pharmaceutical field and the innovation in the food field have inspired a critical pharmaceutical outlook. The active and intelligent packaging for active pharmaceutical ingredients of the future is imagined.

From the pharmaceutical to the clinical: the case for effervescent paracetamol in pain management. A narrative review.

OBJECTIVE: Paracetamol has an established place in the management of mild-to-moderate pain, but has certain limitations, including varying bioavailability, and potential hepatotoxicity if taken in overdose. Effervescent formulations may help to overcome these limitations. METHODS: Pubmed searches, with no limits on date or language, were conducted in February 2020. Further references were identified from the reference lists of retrieved articles, and from the authors' knowledge of the field. RESULTS: Effervescent formulations contain an organic acid (usually citric acid) and carbonate or bicarbonate salts (usually sodium bicarbonate). Upon contact with water, these react to form carbon dioxide, which facilitates the disintegration of the tablet and dissolution of the active drug. Moreover, sodium bicarbonate dose-dependently increases gastric emptying, which together with rapid dissolution facilitates drug absorption. In pharmacokinetic studies, effervescent formulations result in faster absorption of paracetamol than conventional oral formulations, and this translates into a faster onset of analgesia in clinical trials. Effervescent paracetamol has a favorable safety profile, with good tolerability. Importantly, the sodium content of some preparations does not appear to increase cardiovascular risk under real world conditions. Effervescent formulations may also offer advantages in terms of ease of administration and palatability. CONCLUSIONS: Effervescent formulations of paracetamol result in faster drug absorption, and hence more rapid analgesia, than oral tablets, and offer a favorable tolerability and safety profile. The use of such formulations may therefore help to promote appropriate use of paracetamol.

In situ gelling nasal inserts for influenza vaccine delivery.

PURPOSE: The objective of this study was to investigate the potential of rapidly gelling nasal inserts as vaccine delivery system. METHODS: Nasal inserts were prepared by freeze-drying hydrophilic polymer solutions containing influenza split vaccine. In vitro vaccine release from polymer solutions and inserts and the vaccine hemagglutination activity were determined. In vivo immunization studies in mice and rats were performed with nasal solutions and nasal inserts. RESULTS: The in vitro release of proteins (vaccine) from polymeric solutions and inserts was incomplete because of the high molecular weight of the proteins. The release rate was controlled by the polymer (Lutrol F68 > PVP 90 > HPMC K15M > Carbopol > chitosan > or = carrageenan = xanthan gum) because of differences in solution viscosity and possible polymer-protein interactions. Xanthan gum, a negatively charged polymer with intrinsic adjuvanticity, enhanced the serum IgG as well as the nasal IgA response in in vivo studies with nasal vaccine solutions. Poly-l-arginine and cationic lipid were the best performing adjuvants. Solutions containing vaccine with xanthan gum and cationic lipid were effectively stabilized with 0.4 M NaCl. DISCUSSION: The specific activity of the major vaccine protein, hemagglutinin, was not significantly affected by the addition of polymers and the freeze-drying process during insert preparation. The addition of cationic lipid as adjuvant decreased the hemagglutination activity, which strongly indicated inhibition of the protein binding site to erythrocytes. Inserts prepared from xanthan gum and cationic lipid stabilized with NaCl showed a reduced protein activity but were superior to the cationic lipid alone. CONCLUSION: Rat immunization with solid nasal inserts based on xanthan gum containing the influenza vaccine, with or without an additional cationic lipid adjuvant, resulted in similar IgG levels as the pure nasal liquid vaccine formulation.

Preparation and in vitro-in vivo evaluation of salmon calcitonin-loaded polymeric nanoparticles.

The aim of the study was to develop and characterize polymeric nanoparticles as a sustained release system for salmon calcitonin (sCT). Nanoparticles were prepared by a double emulsion solvent evaporation method using Eudragit RS and two types of a biodegradable poly(lactic-co-glycolic) copolymer (PLGA). It was demonstrated that sCT was incorporated into nanoparticles with encapsulation efficiencies in the range 69-83%. In vitro release studies, unconventionally conducted in 5% acetic acid, showed great differences in sCT release time profiles. Nanoparticles with fast release profile (Eudragit RS, PLGA/Eudragit RS) released 80-100% of the encapsulated drug within a few hours. In contrast, the sCT release from pure PLGA nanoparticles was very slow, incomplete and reached only 20% after 4 weeks. In vivo study, conducted in Wistar rats, proved that elevated serum sCT levels could be sustained for 3 days after subcutaneous administration of PLGA nanoparticles and the achieved bioavailability was increased compared to sCT solution.

Pellets for oral administration of low-molecular-weight heparin.

BACKGROUND: Oral absorption of low-molecular-weight heparin (LMWH) is limited by its molecular size and negative charge. It has been shown previously that orally administered polymeric nano- or microparticles containing encapsulated LMWH have led to gastrointestinal absorption of heparin in rabbits. METHOD: Based on these investigations, pellets containing two LMWHs, enoxaparin (MW 4500 Da) or bemiparin (MW 3600 Da), and EudragitRS30D (ERS), were prepared using extrusion/ spheronization technique. Uncoated or coated (ERS) pellets were evaluated in vitro and in vivo on rabbits. RESULTS: Enoxaparin pellets showed fast in vitro release in phosphate buffer (pH 7.4) and prolonged in vivo drug absorption after a single oral dose of 600 anti-Xa IU/ kg of body weight, leading to relative bioavailabilities ranging from 9.7 +/- 1.9% to 12.8 +/- 2.7% and anti-Xa activity over the curative dose. Bemiparin included in matrix pellets of ERS and coated with ERS exhibited in vitro prolonged release up to 4 hours and in vivo anti-Xa activity below the therapeutic minimum value of 0.1 IU/mL. CONCLUSION: This study presents LMWH in a pellet dosage form, which compared to nano- or microparticles, may offer a more convenient and industrializable way of manufacture leading to an easier scale-up process.

Nanoparticle strategies for the oral delivery of insulin.

Since its discovery, insulin remains the major treatment for Type 1 diabetes and many Type 2 diabetic patients, with insulin being administered parenterally. The oral route of insulin delivery, being the most comfortable, would also be the most physiologically advantageous in taking advantage of the portal-hepatic route of absorption. However, insulin is less absorbed by the intestinal mucosa and is rapidly degraded enzymatically in the gastrointestinal tract. Polymeric biodegradable and biocompatible nanoparticles have been developed. These nanoparticles protect insulin against degradation and facilitate the uptake of insulin (associated or not associated to the nanoparticles) through a paracellular or a transcellular pathway. In this review, the physicochemical characteristics of polymer composition, in vitro release kinetics and the biological effects of insulin-loaded nanoparticles in experimental diabetes and healthy animals are discussed.

Increase in the vascular residence time of propranolol-loaded nanoparticles coated with heparin.

Propranolol-HCI incorporated nanoparticles prepared with a blend of a polyester and a polycationic polymer and coated or not with a low molecular weight heparin by electrostatic interactions were prepared by emulsification followed by solvent evaporation. The mean diameter was 388 and 357 nm for coated and uncoated nanoparticles, respectively, and the entrapment efficiency ranged from 20 to 32%. Coated nanoparticles were negatively-charged, whereas uncoated nanoparticles displayed a positive zeta potential (+30 mV). After intravenous administration to rabbits of propranolol-HCI solution and propranolol-loaded nanoparticles coated or not with heparin, pharmacokinetic data revealed that coated nanoparticles exhibited a prolonged blood residence time. It can be concluded that the hydrophilic layer of heparin at the surface of nanoparticles conferred stealth properties which probably reduce the phagocytosis process and avoid immediate uptake by the mononuclear phagocytic system.

Lipid nanoparticles with a solid matrix (SLN, NLC, LDC) for oral drug delivery.

Solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and lipid-drug conjugates (LDC), commonly produced by high-pressure homogenization, are interesting vectors for oral delivery of lipophilic and, to a certain extent, hydrophilic substances. Their production can be done without the use of organic solvents. Techniques to make them a physically stable delivery system have been developed. Scaling up of the production process from lab-size to large-scale dimensions using high-pressure homogenization can be easily achieved by using a different type of homogenizer. The machines used for large-scale production often yield an even better product quality than the lab-scale types. This review article covers the methods of production, characterization, mechanisms of oral bioavailability enhancement, scale-up, final oral dosage forms, and regulatory aspects of lipid nanoparticles for oral drug delivery. It focuses mainly on high-pressure homogenization production methods.

Simple and sensitive HPLC method with fluorescence detection for the measurement of ibuprofen in rat plasma: application to a long-lasting dosage form.

A simple and sensitive high-performance liquid chromatography (HPLC) assay applied to the measurement of ibuprofen in rat plasma has been developed. Two parameters have been investigated to improve ibuprofen detectability using fluorescence detection: variation of mobile phase pH and the use of beta-cyclodextrin (beta-CD). Increasing the pH value from 2.5 to 6.5 and adding 5 mM beta-CD enhanced the fluorescence signal (lambda(exc) = 224 nm; lambda(em) = 290 nm) by 2.5 and 1.3-fold, respectively, when using standards. In the case of plasma samples, only pH variation significantly lowered detection and quantification limits, down to 10 and 35 ng/mL, respectively. Full selectivity was obtained with a single step for plasma treatment, that is, protein precipitation with acidified acetonitrile. The validated method was applied to a pharmacokinetic study of ibuprofen encapsulated in microspheres and subcutaneously administered to rats.

Updated Progress of Nanocarrier-Based Intranasal Drug Delivery Systems for Treatment of Brain Diseases.

Intranasal drug delivery is emerging as a reliable and promising pathway to deliver a wide range of therapeutic agents including small and large molecules, peptides and proteins, genes to the central nervous system for the treatment of brain diseases such as Alzheimer's disease, Parkinson's disease, depression, migraine, schizophrenia, and glioma. This presents noninvasive entry into the brain via direct nose-to-brain and/or indirect nose-to-blood-to-brain routes. Several nanocarrier-based strategies have been developed to transport therapeutic agents to the brain including nanoparticles, liposomes, and exosomes following intranasal delivery. However, the multiple barriers in nose-to-brain route - including rapid mucociliary clearance in the nasal cavity, enzyme degradation, and the blood-brain barrier (BBB) - pose serious challenges to brain-targeted drug delivery. Hence, very limited translation from the laboratory to the clinic has been achieved. The present review highlights the surface modification of nanocarriers with different strategies devoted to facilitate nose-to-brain delivery: prolonging retention time in the nasal cavity, improving penetration ability, and promoting brain targeting with ligands. Additionally, in vitro blood-brain barrier models, influencing an efficient study on intranasal delivery of therapeutics into the brain through indirect nose-to-blood-to-brain pathway, is discussed.

Polymeric Nanoparticles for Increasing Oral Bioavailability of Curcumin.

Despite the promising biological and antioxidant properties of curcumin, its medical applications are limited due to poor solubility in water and low bioavailability. Polymeric nanoparticles (NPs) adapted to oral delivery may overcome these drawbacks. Properties such as particle size, zeta potential, morphology and encapsulation efficiency were assessed. Then, the possibility of storing these NPs in a solid-state form obtained by freeze-drying, in vitro curcumin dissolution and cytocompatibility towards intestinal cells were evaluated. Curcumin-loaded Eudragit® RLPO (ERL) NPs showed smaller particle diameters (245 ± 2 nm) and better redispersibility after freeze-drying than either poly(lactic-co-glycolic acid) (PLGA) or polycaprolactone (PCL) NPs. The former NPs showed lower curcumin encapsulation efficiency (62%) than either PLGA or PCL NPs (90% and 99%, respectively). Nevertheless, ERL NPs showed rapid curcumin release with 91 ± 5% released over 1 h. The three curcumin-loaded NPs proposed in this work were also compatible with intestinal cells. Overall, ERL NPs are the most promising vehicles for increasing the oral bioavailability of curcumin.

Oral delivery of insulin associated to polymeric nanoparticles in diabetic rats.

Nanoparticles prepared with a blend of a biodegradable polyester (poly(-epsilon-caprolactone)) and a polycationic non-biodegradable acrylic polymer (Eudragit RS) have been used as a drug carrier for oral administration of insulin. The rate of encapsulation of insulin was around 96%. The therapeutic efficiency of oral insulin nanoparticles (25, 50 and 100 IU/kg) in diabetic rats and the intestinal uptake of fluorescein isothiocyanate (FITC) labelled insulin were studied. When administered orally by force-feeding to diabetic rats, insulin nanoparticles decreased fasted glycemia in a dose dependant manner with a maximal effect observed with 100 IU/kg. These insulin nanoparticles also increased serum insulin levels and improved the glycemic response to an oral glucose challenge for a prolonged period of time. FITC-Insulin-loaded nanoparticles strongly adhered to the intestinal mucosa and labeled insulin, either released and/or still inside nanoparticles, was mainly taken up by the Peyer's patches. It is concluded that polymeric nanoparticles allows the preservation of insulin's biological activity. In addition, the antidiabetic effect can be explained by the mucoadhesive properties of the polycationic polymer (Eudragit) RS) allowing the intestinal uptake of insulin.

Oral low molecular weight heparin delivery by microparticles from complex coacervation.

As low molecular weight heparins exhibit limited oral absorption they usually have to be administered parenterally. Their strong negative charge appears to be one of the biggest hurdles to overcome in order to increase oral absorption. Complex coacervation has been proposed as a microencapsulation technique for increased oral drug absorption on the basis of charge compensation. Optimized tinzaparin/acacia gum mixture were coacervated with either gelatin A or B leading to microparticles with monodispersed size distribution, good fluidity and high encapsulation rates (>90%), while mean particle size varied between 5 and 20 microm, respectively, depending on the gelatin type. Tinzaparin was homogeneously distributed throughout the particle matrix and anti-Xa activity was maintained during preparation and storage. Drug release occurred in dependency of the pH triggering the dissociation between tinzaparin/acacia and gelatin. Cell binding experiments on Caco-2 led to slightly increased adhesion of gelatin A microparticles compared to gelatin B (A: 3.5+/-0.3%; B: 2.5+/-0.3%; solution: 1.9+/-0.1%), while drug transport did not differ from free tinzaparin solution. In-vivo results demonstrated an oral bioavailability of about 4.2+/-2.9% with gelatin B particles while gelatin A led to no absorption of tinzaparin. In conclusion, tinzaparin microparticles exhibited excellent particle properties in vitro and demonstrate potential for a formulation increasing the oral bioavailability of low molecular weight heparins.

Low molecular weight heparin loaded pH-sensitive microparticles.

Low molecular weight heparins (LMWH) have shown efficacy in the treatment of inflammatory bowel disease after parenteral administration however risking severe hemorrhagic adverse effects. Therefore, an oral colonic targeted heparin dosage form allowing the release of LMWH directly in the inflamed tissue would be of major interest. Enoxaparin was entrapped into pH-sensitive microspheres using Eudragit P4135F that dissolves at pH>7.2. Particle preparation was based on a double emulsion technique with either solvent extraction or evaporation. In order to increase the entrapment efficacy several preparation parameters were optimized, such as inner phase volume, polymer concentration, stabilization of the internal interface by surfactants. Solvent evaporation led to higher entrapment rates (evaporation: 70.1+/-9.9%; extraction: 46.5+/-6.4%). When increasing the volume of the inner aqueous heparin phase, lower encapsulation rates and larger microspheres ( approximately 100-400 microm) were obtained. Sorbitan monostearate (1.75-28% of the total particle mass) had a stabilizing effect on the primary water/oil emulsion. Indeed, higher encapsulation rates (7%: 78.2+/-3.5%; 14%: 76.4+/-10.1%) and smaller particles ( approximately 120-160 microm) were obtained whereas hexadecyltrimethylammonium bromide destabilized the primary emulsion. Interfacial tension studies at a simulated internal water/oil interface confirmed these results. As expected, in vitro drug release was found to be strongly pH-dependent; LMWH was retained in microspheres at pH<6 (<20% release within 4h) whereas a fast drug release was obtained at pH 7.4. The developed microspheres exhibited a particle size adapted to the needs of inflammatory bowel disease therapy, an efficient LMWH encapsulation, and a pH-controlled drug release. These microspheres represent a promising tool for the selective oral delivery of heparin to the colon, especially interesting in the treatment of inflammatory bowel disease.

Impact of bulk and surface properties of some biocompatible hydrophobic polymers on the stability of methylene chloride-in-water mini-emulsions used to prepare nanoparticles by emulsification-solvent evaporation.

The emulsifying and stabilizing ability of several hydrophobic (insoluble in water and soluble in volatile organic solvents) polymers, such as Eudragit RL, Eudragit RS, PLGA, PCL, and their mixtures, with regard to the methylene chloride (MC)-in-water mini-emulsions, has been compared to the viscosity of MC solutions and to the properties of adsorption and spread monolayers of these polymers. Eudragits RS and RL contain approximately 2.5 and approximately 5 mol% of pendent cationic trimethylammonium (TMA) groups per approximately 164 g/mol segments, whereas PLGA and PCL contain 1 and 2 polar carbonyl groups per 130 and 114 g/mol, respectively. The electrostatic attraction between the dipoles, formed by TMA groups and the condensed counter ions in the MC solutions, leads to the contraction of macromolecular coils of Eudragits, whereas the PLGA and PCL macromolecules, interacting by low polar carbonyl groups (with dipole moment mu = 2.7 D) retain more extended conformation in MC. This explains why the characteristic viscosities [eta] of MC solutions are much lower for the former polymers ( approximately 0.1 dL/g) with regard to PLGA and PCL solutions whose [eta] is equal to 0.3 and 0.6 dL/g, respectively. The ionization of TMA groups in contact with the water phase leads to the irreversible adsorption of Eudragits at the MC/water interface and to high decrease of the interfacial tension gamma (down to 4 mN/m for the 5% MC solutions). Whereas PLGA and PCL possessing low polar carbonyl groups adsorb poorly at the MC/water interface exhibiting gamma congruent with 28 mN/m. Higher stability of spread monolayers of Eudragits (pi* approximately 40 mN/m) with regard to PLGA and PCL (pi* < 20 mN/m) correlates well with higher interfacial activity of the former with regard to the later. The higher surface potential DeltaV of Eudragits (0.9 V) with regard to PLGA (0.3 V) and PCL (0.4V) is explained by the formation of electric double layer (DL) by the former, whereas the later contribute to the DeltaV only by cumulative dipole moments of carbonyl groups. The experimental values of surface potentials correlate well with the Gouy-Chapman model of the DL and the Helmholtz model of the monolayer. The ensemble of experimental results leads to the conclusion that higher emulsifying and stabilizing ability of Eudragits with regard to PLGA and PCL is due to higher adsorption activity of the former which form the corona of polymeric chains with ionized TMA groups around the droplets. It can be postulated that Eudragit polymers have good surface active properties which may allow manufacturing of biocompatible nanoparticles by emulsification-solvent evaporation method without surfactants.