Pharmaceutical Advances in Cyclodextrin Inclusion Complexes for Improved Bioavailability of Poorly-Soluble Drugs

2015 ◽  
Vol 8 (3) ◽  
pp. 2894-2905
Author(s):  
Ganesh Raosaheb Godge ◽  
Shivanand Hiremath ◽  
Bhakti Sonawale ◽  
Rani Shirsath
Keyword(s):  
Drug Delivery ◽  
Inclusion Complexes ◽  
Drug Carrier ◽  
Drug Formulation ◽  
Water Soluble ◽  
Formulation Development ◽  
Separation Processes ◽  
Pharmaceutical Application ◽  
Wide Range ◽  
Solubility Enhancers

Cyclodextrins (CDs) are commonly used in drug formulations as solubility enhancers because of their ability to form water-soluble inclusion complexes with poorly water-soluble drugs. Cyclodextrins are useful molecular chelating agents. The cyclodextrins have a wide range of applications in different areas of drug delivery and pharmaceutical industry due to their complexation ability and other versatile characteristics. Orally administered drugs completely absorb only when they show fair solubility in gastric medium and such drugs shows good bioavailability. The solubility and dissolution properties of drugs play an important role in the process of formulation development. The most common pharmaceutical application of cyclodextrin is to enhance the solubility, stability, safety and bioavailability of drug molecules. Cyclodextrins are cyclic oligosaccharides which have recently been recognized as useful pharmaceutical excipients. As a result of molecular complexation phenomena CDs are widely used in many industrial products, technologies and analytical methods. The negligible cytotoxic effects of CDs are an important attribute in applications such as drug carrier, food and flavors, cosmetics, packing, textiles, separation processes, environment protection, fermentation and catalysis. The objective of this review is to discuss and summarize some of the findings and applications of cyclodextrin and their derivatives indifferent areas of drug delivery. The paper also highlights important CD application in drug solubility and dissolution, bioavailability, safety and stability, their use as excipients in drug formulation, design of various novel delivery systems like liposome, microspheres, microcapsules, and nanoparticles. 

scholarly journals Nanoconjugation and Encapsulation Strategies for Improving Drug Delivery and Therapeutic Efficacy of Poorly Water-Soluble Drugs

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 325 ◽  
Author(s):  
Tran ◽  
Tran
Keyword(s):  
Drug Delivery ◽  
Dominant Strategy ◽  
Drug Formulation ◽  
Water Soluble ◽  
Future Application ◽  
Conjugated Materials ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Nanoparticulate Systems

Nanoconjugations have been demonstrated to be a dominant strategy for drug delivery and biomedical applications. In this review, we intend to describe several strategies for drug formulation, especially to improve the bioavailability of poorly water-soluble molecules for future application in the therapy of numerous diseases. The context of current studies will give readers an overview of the conjugation strategies for fabricating nanoparticles, which have expanded from conjugated materials to the surface conjugation of nanovehicles. Moreover, nanoconjugates for theranostics are also discussed and highlighted. Overall, these state-of-the-art conjugation methods and these techniques and applications for nanoparticulate systems of poorly water-soluble drugs will inspire scientists to explore and discover more productive techniques and methodologies for drug development.

scholarly journals Multifunctional NaLnF4@MOF-Ln Nanocomposites with Dual-Mode Luminescence for Drug Delivery and Cell Imaging

Nanomaterials ◽  
2019 ◽  
Vol 9 (9) ◽  
pp. 1274 ◽  
Author(s):  
Wang ◽  
Zhao ◽  
Gao ◽  
Xu ◽  
Wang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cell Imaging ◽  
Drug Carrier ◽  
Drug Carriers ◽  
Water Soluble ◽  
Dual Mode ◽  
Metal Organic ◽  
Lanthanide Metal ◽  
Good Biocompatibility ◽  
Anti Stokes

Multifunctional nanomaterials for bioprobe and drug carrier have drawn great attention for their applications in the early monitoring the progression and treatment of cancers. In this work, we have developed new multifunctional water-soluble NaLnF4@MOF-Ln nanocomposites with dual-mode luminescence, which is based on stokes luminescent mesoporous lanthanide metal–organic frameworks (MOFs-Y:Eu3+) and anti-stokes luminescent NaYF4:Tm3+/Yb3+ nanoparticles. The fluorescence mechanism and dynamics are investigated and the applications of these nanocomposites as bioprobes and drug carriers in the cancer imaging and treatment are explored. Our results demonstrate that these nanocomposites with the excellent two-color emission show great potential in drug delivery, cancer cell imaging, and treatment, which are attributed to the unique spatial structure and good biocompatibility characteristics of NaLnF4@MOF-Ln nanocomposites.

Investigation of Nanoscale Structure of Self-Emulsifying Drug Delivery System Containing Poorly Water-Soluble Model Drug

2014 ◽  
Vol 970 ◽  
pp. 272-278 ◽  
Author(s):  
Mont Kumpugdee-Vollrath ◽  
Yotsanan Weerapol ◽  
Karin Schrader ◽  
Pornsak Sriamornsak
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Correlation Spectroscopy ◽  
Water Soluble ◽  
Wide Range ◽  
Poorly Water Soluble ◽  
Nanoscale Structure ◽  
Model Drug ◽  
20 Nm

This work has a focus on the self-emulsifying drug delivery system (SEDDS), which can be used in pharmaceutical field for increasing bioavailability of poorly water-soluble drugs. The model drug resveratrol was used because of its poor water-solubility and is of interest because of its wide range of pharmacological effects. It is beneficial to understand the mechanism of SEDDS formation in the human body, therefore, the determination of nanoscale structure was carried out. For this purpose, small angle X-ray scattering (SAXS), photon correlation spectroscopy (PCS), and transmission electron microscopy (TEM) techniques were applied. We have found that the size and size distribution of particles were in nanometers. The inner structure of SEDDS was ordered with the lamellar distances (d-spacing) of < 20 nm. It seems that the prepared SEDDS in water form large oil drops (200-400 nm) in water as well as small micelles with the droplet size of 10-20 nm.

scholarly journals Novel Drug Formulation for the Treatment of Hepatic Cancer- A Review

2020 ◽  
Vol 11 (3) ◽  
pp. 4395-4401
Author(s):  
Komala M ◽  
Sathesh Kumar S ◽  
Padmavathy J
Keyword(s):  
Drug Delivery ◽  
Polar Lipid ◽  
Self Assembly ◽  
Drug Carrier ◽  
Global Market ◽  
Drug Formulation ◽  
Drug Uptake ◽  
Bioactive Materials ◽  
The Core ◽  
Regenerative Medicines

For metabolic transformation, uptake, detoxification, and excretion liver is the primary organ that is highly equipped. Thus, the liver requires targeting by means like a carrier-mediated mechanism to take xenobiotics into the bile, though high hepatic concentration is achieved by most of the drugs. Thus resulting in high first-pass metabolism displayed by the drugs and thus resulting in rapid clearance of the drugs. Uptake of particulate materials is highly contributed by the kupffer cells largely. However, drug uptake by the liver is highly dependent on hepatocytes. In drug delivery, tissue engineering and regenerative medicines which are various biomedical applications construction of nanoscale based bioactive materials is a desirable approach of self-assembly. By using a targeting moiety, we can decrease the side effects of the drug and increases the therapeutic effect of the drug. Lipoproteins are potential drug carrier to target the organs. Lipoproteins consist of cholesterol, polar lipid core surrounding phospholipid monolayer and apoproteins are embedded in it, and these lipoproteins are spherical. The core is a polar lipid in nature so that highly hydrophobic drugs are easily incorporated into the core. Lipoproteins are completely non-immunogenic, biodegradable nature. The present review should be regularly inspected to beat into the global market at an affordable price as well, particularly the vehicles which are proven to be efficacious in drug delivery systems used to treat liver diseases like cancer.

scholarly journals Σύνθεση και χαρακτηρισμός πρωτότυπων ολιγομερών κυκλοδεξτρινών για μεταφορά φαρμάκων

2014 ◽  
Author(s):  
Μαλαματένια Μανουηλίδου
Keyword(s):  
Binding Capacity ◽  
Drug Carrier ◽  
Aqueous Solubility ◽  
Single Step ◽  
Drug Formulation ◽  
Water Soluble ◽  
Amide Bond ◽  
Mild Conditions ◽  
Order Of Magnitude ◽  
High Yields

Cyclodextrins (CDs) are cyclic hollow oligosaccharide molecules that form water solublehost-guest systems, with many applications in drug formulation and delivery. CDoligomers have been previously studied due to the interest towards smart hosts withenhanced molecular recognition and binding capacity as sensors, catalysts, enzymemimics, photoreactive systems, etc. The aim of this dissertation was to prepare αCDoligomers for drug inclusion and transport with criteria: (i) ease of preparation, inaqueous media, in short steps, under mild conditions and in good yields, (ii) to obtainoligomers with satisfactory aqueous solubility and full availability of the CD cavities (iv)to achieve multiple binding with strengths better or comparable to those of parent αCD.The copper catalyzed azide-alkyne cyclization (CuAAC) reaction was utilized to preparea new water soluble cyclodextrin trimer very efficiently. The trimer engulfed threemolecules of a model guest and satisfactorily solubilized the chemotherapeutictamoxifen citrate and its active metabolite, N-desmethyltamoxifen, increasing theirsolubility by >1 order of magnitude. Moreover, for the first time the bioorthogonalStaudinger Ligation was applied to prepare αCD-dimers. For this purpose, a doublyactive linker was specifically developed that enabled dimer preparation in a single step,in aqueous/organic media, under mild conditions and with high yields. The aboveprepared products were studied in detail by NMR spectroscopy and were found toadopt, by self-inclusion, a closed conformation in aqueous solution, which completelyopened up in the presence of a suitable guest, leaving the cavities fully available to formthe corresponding inclusion complexes. Titration and DOSY NMR experimentsconfirmed the above and showed that the dimeric species form slowly diffusingaggregates in water, that in the presence of the guest partially disperse. The StaudingerLigation could thus become the method of choice for preparing CD dimers.Solubilization of practically insoluble N-desmethyl-tamoxifen was also achieved to 0.3mM. Moreover, CD dimers prepared via amide bond formation were less efficient andrequired harsh conditions. Finally, SNO-αCD derivatives were prepared andcharacterized as bimodal NO and drug carrier systems.

scholarly journals PROPERTIES, PHARMACEUTICAL APPLICATION AND VARIOUS TECHNIQUE OF CHEMICAL MODIFICATION IN NATIVE STARCH: A DESCRIPTIVE REVIEW

2019 ◽  
pp. 54-59
Author(s):  
BISHAL JYOTI BORDOLOI ◽  
BHUPEN KALITA ◽  
DIBYENDU SHIL
Keyword(s):  
Drug Delivery ◽  
Chemical Modification ◽  
The Body ◽  
Gelling Agent ◽  
Intrinsic Properties ◽  
Pharmaceutical Application ◽  
Conventional Drug ◽  
Wide Range ◽  
Thickening Power ◽  
And Storage

Starch is one important natural polymer that finds application in the formulation of dosage forms as the binder, disintegrates, diluents, gelling agent etc. Starch is drawing the attention in drug delivery as it is cheap, non-toxic, renewable, biodegradable and compatible with many other materials for industrial application. Starch has vital intrinsic properties that have made its pharmaceutical applications possible. It has also been used for a wide range of particular drug delivery applications, such as the delivery of challenging molecules and targeting to specific sites in the body. Starches are integrally unsuitable for most applications such as loss of viscosity and thickening power upon cooking and storage, retrogradation characteristics and absence of certain groups responsible for a particular function etc. So, in order to reduce its limitations and improve its applications, modification of starch is necessary. It can be modified by several ways like chemical modification, physical modification and genetic modification but the most important one is the chemical modification. This review summarizes the properties and application of native starchin conventional drug delivery systems within a world of dynamic drug production technology. It also describes the chemical modification like cross-linking, esterification, etherification and dual modification of starch.

Recent Advances in Solid Dispersion Technology for Efficient Delivery of Poorly Water-Soluble Drugs

2019 ◽  
Vol 25 (13) ◽  
pp. 1524-1535 ◽  
Author(s):  
Gourav Paudwal ◽  
Neha Rawat ◽  
Rahul Gupta ◽  
Ashish Baldi ◽  
Gurdarshan Singh ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Solid Dispersion ◽  
Oral Drug Delivery ◽  
Water Soluble ◽  
Attrition Rate ◽  
Synthetic Methods ◽  
Oral Drug ◽  
Screening Methods ◽  
Formulation Development ◽  
Poorly Water Soluble

Drug discovery is generally considered as a costly affair and it takes approximately 15 years to reach a new chemical entity into the market. Among the recent potent drug molecules with most effective pharmacological properties, very few reached for Phase I clinical trial in humans. Unfortunately, the historical average reveals an almost 90% overall attrition rate in clinical trials. The solubility and permeability of a drug are the critical factors influencing the success of a drug. Oral drug delivery systems still continue to exist as the most favored, simplest and easiest administration route. A huge number of potential clinical candidates won’t make it to the market or accomplish their maximum capacity except if their solubility and oral bioavailability are enhanced by formulation. The solubility of drugs will continue to exist as important aspects of formulation development. With the emergence of synthetic methods for new molecule synthesis in chemistry and better screening methods, the number of poorly water soluble compounds has dramatically expanded in the last few years. Solid dispersion is one of the most important techniques as it can be prepared by several methods. It is mostly prepared with a drug having poor water solubility and it explores hydrophilic polymers either individually or in combination for the enhancement of solubility. In comparison to the conventional formulations such as tablets or capsules, there are different methods with which solid dispersions can be prepared and also have many benefits over conventional drug delivery approaches. Solid dispersion systems are potential for increasing the solubility, oral absorption and bioavailability of drugs and the significance of the solid dispersion technology is constantly increasing. The main focus of this review is to present recent advancements in the area of solid dispersion. This review also includes an account of recent patents on solid dispersion and clinical status of solid dispersion based formulations.

CYCLODEXTRIN IN DRUG DELIVERY APPLICATION: A REVIEW

2019 ◽  
Vol 7 (4) ◽  
Author(s):  
Rajveer Bhaskar ◽  
Monika Ola ◽  
Rahul Patel ◽  
Dr. S. S. Chalikwar
Keyword(s):  
Drug Delivery ◽  
High Performance ◽  
Pulmonary Delivery ◽  
Drug Carriers ◽  
Review Article ◽  
Complexing Agents ◽  
Nasal Drug Delivery ◽  
Drug Molecules ◽  
Pharmaceutical Application ◽  
Wide Range

The cyclodextrins have a wide range of applications in various areas of drug delivery and pharmaceutical industry due to their complexation ability and other versatile characteristics. The most popular pharmaceutical application of cyclodextrin is to increase the solubility, stability, safety and bioavailability of drug molecules. The idea of this review article is to solve and study any of the findings and application of cyclodextrin (CD) and their derivatives in different areas of drug delivery. This review article introduce the molecular structure, properties like complexation, solubility etc. of cyclodextrins and targeted on its use for parenteral, oral, ophthalmic and nasal drug delivery. Other routes including dermal, rectal, sublingual and pulmonary delivery are again briefly addressed. The aim of this contribution is to focus on the potential application of chemically altared cyclodextrins as high-performance drug carriers in drug delivery systems with emphasis on the other recent developments. Thus cyclodextrins, because of their continuing ability to find several novel applications in drug delivery, are expected to solve many problems associated with the delivery of different other novel drugs through different delivery routes. Keywords: Cyclodextrin, complexing agents, bioavailability, industrial application

scholarly journals Drug Delivery Nanoparticles in Skin Cancers

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Chiara Dianzani ◽  
Gian Paolo Zara ◽  
Giovanni Maina ◽  
Piergiorgio Pettazzoni ◽  
Stefania Pizzimenti ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cell Carcinoma ◽  
Materials Science ◽  
Drug Carrier ◽  
Water Soluble ◽  
Cancer Disease ◽  
Research Areas ◽  
Tunable Release ◽  
Water Soluble Drugs ◽  
Active Research

Nanotechnology involves the engineering of functional systems at nanoscale, thus being attractive for disciplines ranging from materials science to biomedicine. One of the most active research areas of the nanotechnology is nanomedicine, which applies nanotechnology to highly specific medical interventions for prevention, diagnosis, and treatment of diseases, including cancer disease. Over the past two decades, the rapid developments in nanotechnology have allowed the incorporation of multiple therapeutic, sensing, and targeting agents into nanoparticles, for detection, prevention, and treatment of cancer diseases. Nanoparticles offer many advantages as drug carrier systems since they can improve the solubility of poorly water-soluble drugs, modify pharmacokinetics, increase drug half-life by reducing immunogenicity, improve bioavailability, and diminish drug metabolism. They can also enable a tunable release of therapeutic compounds and the simultaneous delivery of two or more drugs for combination therapy. In this review, we discuss the recent advances in the use of different types of nanoparticles for systemic and topical drug delivery in the treatment of skin cancer. In particular, the progress in the treatment with nanocarriers of basal cell carcinoma, squamous cell carcinoma, and melanoma has been reported.

scholarly journals Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

2012 ◽  
Vol 62 (4) ◽  
pp. 563-580 ◽  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Systemic Exposure ◽  
Tween 80 ◽  
Water Soluble ◽  
Formulation Development ◽  
Suspension Formulation ◽  
Water Soluble Drugs

The aim of the study was to develop and evaluate a self- -emulsifying drug delivery system (SEDDS) formulation to improve solubility and dissolution and to enhance systemic exposure of a BCS class II anthelmetic drug, albendazole (ABZ). In the present study, solubility of ABZ was determined in various oils, surfactants and co-surfactants to identify the microemulsion components. Pseudoternary phase diagrams were plotted to identify the microemulsification existence area. SEDDS formulation of ABZ was prepared using oil (Labrafac Lipopfile WL1349) and a surfactant/ co-surfactant (Tween 80/PEG 400) mixture and was characterized by appropriate studies, viz., microemulsifying properties, droplet size measurement, in vitro dissolution, etc. Finally, PK of the ABZ SEDDS formulation was performed on rats in parallel with suspension formulation. It was concluded that the SEDDS formulation approach can be used to improve the dissolution and systemic exposure of poorly water-soluble drugs such as ABZ.

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