scholarly journals A Customized Screening Tool Approach for the Development of a Self-Nanoemulsifying Drug Delivery System (SNEDDS)

2021 ◽  
Vol 23 (1) ◽  
Author(s):  
Fabian-Pascal Schmied ◽  
Alexander Bernhardt ◽  
Andrea Engel ◽  
Sandra Klein
Keyword(s):  
Drug Delivery ◽  
Screening Tool ◽  
Aqueous Solubility ◽  
Mapping Method ◽  
Mixture Design ◽  
Characterization Methods ◽  
Strategic Approach ◽  
Performance Results ◽  
Short Time

AbstractThe present study focused on establishing a novel, (pre-)screening approach that enables the development of promising performing self-nanoemulsifying drug delivery systems (SNEDDSs) with a limited number of experiments. The strategic approach was based on first identifying appropriate excipients (oils/lipids, surfactants, and co-solvents) providing a high saturation solubility for lipophilic model compounds with poor aqueous solubility. Excipients meeting these requirements were selected for SNEDDS development, and a special triangular mixture design was applied for determining excipient ratios for the SNEDDS formulations. Celecoxib and fenofibrate were used as model drugs. Formulations were studied applying a specific combination of in vitro characterization methods. Specifications for a promising SNEDDS formulation were self-imposed: a very small droplet size (< 50 nm), a narrow size distribution of these droplets (PDI < 0.15) and a high transmittance following SNEDDS dispersion in water (> 99% in comparison with purified water). Excipients that provided a nanoemulsion after dispersion were combined, and ratios were optimized using a customized mapping method in a triangular mixture design. The best performing formulations were finally studied for their in vitro release performance. Results of the study demonstrate the efficiency of the customized screening tool approach. Since it enables successful SNEDDS development in a short time with manageable resources, this novel screening tool approach could play an important role in future SNEDDS development.

Enhanced Oral Bioavailability and Improved Biological Activities of a Quercetin/Resveratrol Combination Using a Liquid Self-Microemulsifying Drug Delivery System

Planta Medica ◽  
2020 ◽  
Author(s):  
Patcharawalai Jaisamut ◽  
Subhaphorn Wanna ◽  
Surasak Limsuwan ◽  
Sasitorn Chusri ◽  
Kamonthip Wiwattanawongsa ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Biological Activities ◽  
Area Under The Curve ◽  
Aqueous Solubility ◽  
The Self

AbstractBoth quercetin and resveratrol are promising plant-derived compounds with various well-described biological activities; however, they are categorized as having low aqueous solubility and labile natural compounds. The purpose of the present study was to propose a drug delivery system to enhance the oral bioavailability of combined quercetin and resveratrol. The suitable self-microemulsifying formulation containing quercetin together with resveratrol comprised 100 mg Capryol 90, 700 mg Cremophor EL, 200 mg Labrasol, 20 mg quercetin, and 20 mg resveratrol, which gave a particle size of 16.91 ± 0.08 nm and was stable under both intermediate and accelerated storage conditions for 12 months. The percentages of release for quercetin and resveratrol in the self-microemulsifying formulation were 75.88 ± 1.44 and 86.32 ± 2.32%, respectively, at 30 min. In rats, an in vivo pharmacokinetics study revealed that the area under the curve of the self-microemulsifying formulation containing quercetin and resveratrol increased approximately ninefold for quercetin and threefold for resveratrol compared with the unformulated compounds. Moreover, the self-microemulsifying formulation containing quercetin and resveratrol slightly enhanced the in vitro antioxidant and cytotoxic effects on AGS, Caco-2, and HT-29 cells. These findings demonstrate that the self-microemulsifying formulation containing quercetin and resveratrol could successfully enhance the oral bioavailability of the combination of quercetin and resveratrol without interfering with their biological activities. These results provide valuable information for more in-depth research into the utilization of combined quercetin and resveratrol.

scholarly journals Albumin coated liposomes: a novel platform for macrophage specific drug delivery

2011 ◽  
Vol 1 (1) ◽  
pp. 2 ◽  
Author(s):  
Clément Vuarchey ◽  
Sushil Kumar ◽  
Reto Schwendener
Keyword(s):  
Drug Delivery ◽  
Drug Carrier ◽  
Cell Types ◽  
Specific Drug ◽  
Splenic Macrophages ◽  
Peg Liposomes ◽  
Short Time ◽  
Liposome Surface

Here we report a new and efficient approach of macrophage specific drug delivery by coating liposomes with albumin. Activated albumin was reacted with liposomes containing polyethylene glycol (PEG) as hydrophilic spacers to create a flexible layer of covalently bound albumin molecules on the liposome surface. Albumin coated liposomes were taken up faster and more efficiently than uncoated liposomes by murine macrophages. Liposome uptake was significantly higher in macropha - ges as compared to other cell types tested (endothelial cells, fibroblasts, tumor cells), suggesting specificity for macrophages. In vivo, splenic macrophages phagocytosed BSA coated liposomes (BSA-L) at faster rates compared to conventional liposomes (L) and PEG liposomes (PEG-L). To prove the effectiveness of this new macrophage specific drug carrier, the bisphosphonates clodronate and zoledronate were encapsulated in BSA-L and compared with conventional liposomes. <em>In vitro</em>, treatment of macrophages with clodronate or zoledronate in BSA-L led to cytotoxic activity within a very short time and to up to 50-fold reduced IC50 concentrations. <em>In vivo</em>, clodronate encapsulated in BSA-L depleted splenic macrophages at a 5-fold lower concentration as conventional clodronate-liposomes. Our results highlight the pharmaceutical benefits of albumin-coated liposomes for macrophage specific drug delivery.

scholarly journals In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility

2021 ◽  
Vol 14 (11) ◽  
pp. 1089
Author(s):  
Hakan Nazlı ◽  
Burcu Mesut ◽  
Yıldız Özsoy
Keyword(s):  
Drug Delivery ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Ternary Phase Diagrams ◽  
Enhanced Solubility ◽  
Porous Carriers ◽  
Drug Precipitation ◽  
Precipitation Inhibitors ◽  
Preformulation Studies

Aprepitant (APR) belongs to Class II of the Biopharmaceutical Classification System (BCS) because of its low aqueous solubility. The objective of the current work is to develop self-nanoemulsifying drug delivery systems (SNEDDS) of APR to enhance its aqueous solubility. Preformulation studies involving screening of excipients for solubility and emulsification efficiency were carried out. Pseudo ternary phase diagrams were constructed with blends of oil (Imwitor® 988), cosolvent (Transcutol® P), and various surfactants (Kolliphor® RH40, Kolliphor® ELP, Kolliphor® HS15). The prepared SNEDDS were characterized for droplet size and nanoemulsion stability after dilution. Supersaturated SNEDDS (super-SNEDDS) were prepared to increase the quantity of loaded APR into the formulations. HPMC, PVP, PVP/VA, and Soluplus® were used as polymeric precipitation inhibitors (PPI). PPIs were added to the formulations at 5% and 10% by weight. The influence of the PPIs on drug precipitation was investigated. In vitro lipolysis test was carried out to simulate digestion of formulations in the gastrointestinal tract. Optimized super-SNEDDS were formulated into free-flowing granules by adsorption on the porous carriers such as Neusilin® US2. In vitro dissolution studies of solid super-SNEDDS formulation revealed an increased dissolution rate of the drug due to enhanced solubility. Consequently, a formulation to improve the solubility and potentially bioavailability of the drug was developed.

scholarly journals Interaction Between Chitosan and Mucin: Fundamentals and Applications

Biomimetics ◽  
2019 ◽  
Vol 4 (2) ◽  
pp. 32 ◽  
Author(s):  
Collado-González ◽  
González Espinosa ◽  
Goycoolea
Keyword(s):  
Drug Delivery ◽  
Chemical Structure ◽  
Molecular Level ◽  
Ex Vivo ◽  
Biological Properties ◽  
Characterization Methods ◽  
Variable Chemical ◽  
And Behavior ◽  
Structure Properties

The term chitosan (CS) refers to a family of aminopolysaccharides derived from chitin. Among other properties, CS is nontoxic, mucoadhesive and can be used for load and transport drugs. Given these and other physicochemical and biological properties, CS is an optimal biopolymer for the development of transmucosal drug delivery systems, as well as for the treatment of pathologies related to mucosal dysfunctions. Mucins are glycoprotein macromolecules that are the major components of mucus overlaying epithelia. CS interacts with mucin and adsorbs on and changes the rheology of mucus. However, CS and mucins denote families of polymers/macromolecules with highly variable chemical structure, properties, and behavior. To date, their interactions at the molecular level have not been completely unraveled. Also, the properties of complexes composed of CS and mucin vary as a function of the sources and preparation of the polymers. As a consequence, the mucoadhesion and drug delivery properties of such complexes vary as well. The breadth of this review is on the molecular interactions between CS and mucin. In particular, in vitro and ex vivo characterization methods to investigate both the interactions at play during the formation of CS-mucin complexes, and the advances on the use of CS for transmucosal drug delivery are addressed.

scholarly journals Preparation and In vitro Characterization of Aceclofenac Nanosuspension (ACNS) for Enhancement of Percutaneous Absorption using Hydrogel Dosage Form

2021 ◽  
Vol 30 (2) ◽  
pp. 86-98
Author(s):  
Aseel Kadhem Thamer ◽  
Ahmed Najem Abood
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Physical Stability ◽  
Methyl Cellulose ◽  
Aqueous Solubility ◽  
Vinyl Pyrrolidone ◽  
Precipitation Method ◽  
Characterization Methods ◽  
Anti Inflammatory

         Aceclofenac (AC) is an orally active phenyl acetic acid derivative, non-steroidal anti-inflammatory drug with exceptional anti-inflammatory, analgesic and antipyretic properties. It has low aqueous solubility, leading to slow dissolution, low permeability and inadequate bioavailability. The aim of the current study was to prepare and characterize AC-NS-based gel to enhance the dissolution rate and then percutaneous permeability. NS.s were prepared using solvent/antisovent precipitation method at different drug to polymer ratios (1:1, 1:2, and 1:3) using different polymers such as poly vinyl pyrrolidone (PVP-K25), hydroxy propyl methyl cellulose (HPMC-E5) and poloxamer® (388) as stabilizers alone and in combinations of two polymers (1:2 and 1:4 Drug: polymer ratio). Fifteen formulas of AC-NS.s were prepared and characterized for production yield, loading efficiency, particle size, polydispersity index and physical stability. The best formulas of NS were then lyophilized to be characterized by FTIR, DSC, P-XRD and SEM. After that, the best prepared formula of AC-NS regarding the involved characterization methods was incorporated in gel dosage forms using carbopol®940. From this study, we conclude that the dissolution rate and permeability of AC were improved when the particle size was reduced to Nano-scale as compared with pure drug.

scholarly journals A Review on Characterizations and Biocompatibility of Functionalized Carbon Nanotubes in Drug Delivery Design

2014 ◽  
Vol 2014 ◽  
pp. 1-20 ◽  
Author(s):  
Julia M. Tan ◽  
Palanisamy Arulselvan ◽  
Sharida Fakurazi ◽  
Hairuszah Ithnin ◽  
Mohd Zobir Hussein
Keyword(s):  
Carbon Nanotubes ◽  
Drug Delivery ◽  
Surface Modification ◽  
Chemical Properties ◽  
Analytical Techniques ◽  
Aqueous Environment ◽  
Functionalized Carbon Nanotubes ◽  
Characterization Methods ◽  
Physical And Chemical

The revolutionary development of functionalized carbon nanotubes (f-CNTs) for applications in nanomedicine has emerged as one of the most interesting fields, which has increased exponentially in recent years. This is due to their appealing physical and chemical properties, as well as their unique architecture. After a brief introduction on the physicochemical properties of carbon nanotubes (CNTs), we described several functionalization methods for the surface modification of CNTs, with the aim to facilitate their solubility in physiological aqueous environment. This review focuses on recent advances in drug delivery design based onf-CNTs with an emphasis on the determination of various parameters involved and characterization methods used in order to achieve higher therapeutic efficacy of targeted drug delivery. In particular, we will highlight a variety of different analytical techniques which can be used to characterize the elemental composition, chemical structure, and functional groups introduced onto the CNTs after surface modification. We also review the current progress of availablein vitrobiocompatibility assays based onf-CNTs and then discuss their toxicological profile and biodistribution for advanced drug delivery.

Application of D-optimal mixture design for development and optimization of Olmesartan Medoxomil loaded SMEDDS

2020 ◽  
Vol 15 ◽  
Author(s):  
Navdeep Gahlawat ◽  
Ravinder Verma ◽  
Deepak Kaushik
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Olmesartan Medoxomil ◽  
Mixture Design ◽  
In Vitro Dissolution ◽  
Angiotensin Ii Receptor Blocker ◽  
Globule Size

Background: Olmesartan medoxomil is an angiotensin II receptor blocker antihypertensive drug which has low oral bioavailability because of poor aqueous solubility. Objective: The objective of present research is development and optimization of Olmesartan medoxomil loaded self-microemulsifying drug delivery system by D-optimal mixture design to improve its dissolution rate. Methods: Solubility of Olmesartan medoxomil was determined in different oils, surfactants and co-surfactants. Pseudo ternary diagram was constructed for identification of self-microemulsification region. The D-optimal mixture design was employed for optimization of SMEDDS formulations wherein the factors optimized were the concentration of oil (X1), surfactant (X2) and co-surfactant (X3) and the response were globule size (Y1) and dissolution rate (Y2). Developed self-microemulsifying drug delivery system were further assessed for self-emulsification time, drug loading capacity, transparency, globule size, in vitro dissolution and comparative in vitro dissolution testing of optimized formulation with pure medicament and commercially available product. Results: The application of D-optimal mixture design resulted in 14 batches out of which F-5 was found to be the optimized batch which contained Olmesartan medoxomil (20 mg), Capmul MCM EP (23% v/v), Kolliphore EL (49% v/v) and Transcutol P (28% v/v) having globule size of 105 nm, 94.7% dissolution within 30 minutes. In vitro dissolution rate of the drug from SMEDDS was appreciably higher than that of pure drug and marketed product. Conclusion: Olmesartan medoxomil self-microemulsifying drug delivery system was successfully developed and this approach could prove to be suitable for improvement of dissolution rate of BCS II class drugs.

scholarly journals Preparation and Evaluation of Zafirlukast Compression Coated Tablets for Chronotherapeutic Drug Delivery

2021 ◽  
pp. 154-166
Author(s):  
M. S. Neeharika ◽  
B. Jeevana Jyothi
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Solid Dispersion ◽  
Chemical Interaction ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Natural Polymers ◽  
Compression Coating

The objective of the present study was to formulate and evaluate an oral, time-controlled drug delivery system of Zafirlukast. Zafirlukast belongs to BCS class II drugs as it has poor aqueous solubility and good permeability. Hence an attempt has been made to improve its aqueous solubility by solid dispersion technique so that its dissolution, bioavailability, and therapeutic effect can be optimized. The optimized solid dispersion was then formulated into a chronotherapeutic drug delivery system by compression coating technology. FT-IR study revealed that there was no chemical interaction between the drug and polymers used. Tablets were prepared by direct compression method using different super disintegrants and then followed by compression coating using natural polymers. Pre-compression and post-compression parameters complied with the Pharmacopoeia limit for the tablets. In vitro release studies were performed and the results indicated the formulation Z9F9 to be the optimized formulation.

In-Vitro and In-Vivo Evaluation of Supersaturable Self-Nanoemulsifying Drug Delivery System (SNEDDS) of Dutasteride

2020 ◽  
Vol 17 (1) ◽  
pp. 74-86 ◽  
Author(s):  
Poonguzhali Subramanian ◽  
P. S. Rajnikanth ◽  
Manish Kumar ◽  
Kumarappan Chidambram
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Absorption ◽  
Drug Loading ◽  
Methyl Cellulose ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Drug Load

Objective: A novel, Supersaturable Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) has been prepared to improve the Dutasteride's poor aqueous solubility. Methods: By adding Hydroxy Propyl Methyl Cellulose (HPMC) as a precipitation inhibitor to conventional SNEDDS, a supersaturable system was prepared. Firstly, the prepared SNEDDS played an important role in increasing the aqueous solubility and hence oral absorption due to nano-range size. Secondly, the S-SNEDDS found to be advantageous over SNEDDS for having a higher drug load and inhibition of dilution precipitation of Dutasteride. Formulated S-SNEDDS (F1-F9) ranged from 37.42 ± 1.02 to 68.92 ± 0.09 nm with PDI 0.219-0.34 and drug loading of over 95 percent. Results: The study of in-vitro dissolution revealed higher dissolution for S-SNEDDS compared to SNEDDS and Avodart soft gelatin capsule as a commercial product. In addition, higher absorption was observed for S-SNEDDS showing approximately 1.28 and 1.27 fold AUC (0-24h) and Cmax compared to commercial products. Therefore, S-SNEDDS has proven as a novel drug delivery system with a higher drug load, higher self-emulsification efficiency, higher stability, higher dissolution and pronounced absorption. Conclusion: In conclusion, S-SNEDDS could be a new emerging approach to enhance aqueous solubility in many folds for drugs belonging to BCS Class II and IV and thus absorption and oral bioavailability.

Preparation of Atorvastatin Loaded Chitosan Nanoparticles: In Vitro and In Vivo Evaluations

2020 ◽  
Vol 19 (05) ◽  
pp. 1950036
Author(s):  
V. Lavanya ◽  
P. Rajeswari ◽  
M. Vidyavathi ◽  
R. V. Sureshkumar
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Low Cost ◽  
Chitosan Nanoparticles ◽  
Hdl Cholesterol ◽  
Aqueous Solubility ◽  
Loading Efficiency ◽  
Significant Difference

This study is aimed at the preparation and evaluation of atorvastatin (AN)-loaded chitosan (CS) nanoparticles to achieve improved bioavailability of atorvastatin as its bioavailability is very poor. Chitosan is a popular choice in the application as a drug delivery carrier due to its biocompatibility, chemical versatility, aqueous solubility and low cost. Hence, a total of nine formulations (AN1–AN9) were prepared to study the effects of CS:tripolyphosphate (TPP) ratio and the amount of drug. The best formulation was selected by calculating the overall desirability (OD) factor. Among all, AN9 was found to possess the maximum percentage yield, loading efficiency and percentage (%) drug release compared to other formulations due to the incorporation of more amount of polymer compared to other formulations. SEM microphotographs and zeta-sizer reports indicated that atorvastatin-loaded chitosan nanoparticles were in the nanometric range and were spherical, discrete and uniform in size. The selected polymer chitosan was found to possess good compatibility with atorvastatin, without any mutual interaction, based on the results of DSC and FTIR analyses. The nanoparticles were found to have good flow properties. The in vivo results proved that the best formulation has shown significant difference in the reduction of triglycerides (TG), total cholesterol (TC) and no significant change in high density lipids (HDL) cholesterol levels in blood when compared with the marketed formulation. Better regenerative changes were observed during histopathological evaluation of liver in a group treated with atorvastatin nanoparticles than those of other groups, that confirmed the improved hypolipidemic action. Thus, from all the above observations, it was concluded that AN9 formulation has shown the highest in vitro drug release and loading efficiency than other formulations, which might be due to increased entrapment of drug and the surface area through decreased particle size which further confirmed the improved in vitro bioavailability and in vivo performance than those of marketed atorvastatin tablet. This study strongly suggests the use of chitosan nanoparticles as drug delivery system to improve the bioavailability of atorvastatin.

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