Design, Optimization and Evaluation of Lurasidone Hydrochloride Nanocrystals as Fast Disintegrating Tablets

2019 ◽  
Vol 4 (2) ◽  
pp. 121-129
Author(s):  
Satya Sankar Sahoo ◽  
Chandu Babu Rao
Keyword(s):  
Patient Compliance ◽  
Oral Drug Delivery ◽  
Particle Diameter ◽  
Water Soluble ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Water Soluble Drugs ◽  
Fast Disintegrating Tablets ◽  
Lurasidone Hydrochloride

Formulation of poorly water-soluble drugs for oral drug delivery has always been a difficult task for formulation scientists. Lurasidone hydrochloride is one such agent which is used to control bipolar depre-ssion. The objective of this study was to formulate and optimize lurasi-done nanosuspension, further formulating optimized nanosuspensions as fast disintegrating tablets for improved patient compliance. In the present study, lurasidone nanosuspension was prepared by nanomilling technique. Optimized nanosuspension has mean particle diameter of 248.9 nm, polydispersity index of 0.127 and zeta potential of 18.1 mV. The lyophilized optimized nanocrystals, optimize nanosuspension as granulating fluid and as top spraying dispersion for granulation in fluid bed granulator being used to formulate fast disintegrating tablets with suitable super disintegrant. Croscarmellose sodium was found to be best superdisintegrant compared to sodium starch glycolate and crospovidone, as its acts by both mechanism swelling and wicking. Its swells 4-8 folds in less than 10 s. Many folds increase in the rate of drug release observed compare to micronized lurasidone and marketed product. There was no change in crystalline nature after nanomilling as characterized by XRD and FTIR, and it was found to be chemically stable with high drug content. The developed fast disintegrating tablets would be an alternative better formulation than its conventional formulation to address its bioavailability issue and for improved patient compliance. However, this should be further confirmed by appropriate in vivo studies.

What is the future for nanocrystal-based drug-delivery systems?

2020 ◽  
Vol 11 (4) ◽  
pp. 225-229 ◽  
Author(s):  
Zhongjian Chen ◽  
Wei Wu ◽  
Yi Lu
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Water Soluble ◽  
Oral Drug ◽  
Particle Properties ◽  
Novel Approach ◽  
The Future ◽  
Water Soluble Drugs ◽  
Delivery Platform

Nanocrystals are used as a drug-delivery platform for poorly water-soluble drugs and have had commercial success in oral drug delivery. We assert that the future of this technique is with cancer treatment and in the development of parenteral preparations. Advances in techniques for uniform and high-quality nanocrystals as well as deciphering the in vivo fate of nanocrystals are critical. The bottom-up technique allows for better control of particle properties, while the hybrid nanocrystal technique provides a novel approach to explore the in vivo fate of nanocrystals. Breakthroughs in these two techniques to further the development of nanocrystals are also discussed.

Ionic liquids provide unique opportunities for oral drug delivery: structure optimization and in vivo evidence of utility

2014 ◽  
Vol 50 (14) ◽  
pp. 1688-1690 ◽  
Author(s):  
Hywel D. Williams ◽  
Yasemin Sahbaz ◽  
Leigh Ford ◽  
Tri-Hung Nguyen ◽  
Peter J. Scammells ◽  
...  
Keyword(s):  
Prolonged Exposure ◽  
Oral Drug Delivery ◽  
Structure Optimization ◽  
Water Soluble ◽  
Oral Drug ◽  
Poorly Water Soluble Drugs ◽  
Custom Made ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Custom-made ILs solubilized high quantities of the poorly water-soluble drugs, danazol and itraconazole, while a danazol self-emulsifying IL formulation gave rise to higher and more prolonged exposure than the crystalline drug and a lipid formulation, respectively.

In vitro and in vivo studies of enzyme-digestible hydrogels for oral drug delivery

1992 ◽  
Vol 19 (1-3) ◽  
pp. 131-144 ◽  
Author(s):  
Waleed S.W. Shalaby ◽  
William E. Blevins ◽  
Kinam Park
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
In Vivo Studies ◽  
Oral Drug

scholarly journals ENHANCING OF ORAL BIOAVAILABILITY OF POORLY WATER-SOLUBLE ANTIHYPERTENSIVE DRUGS

2021 ◽  
pp. 42-47
Author(s):  
BITOPAN BAISHYA ◽  
SHEIKH SOFIUR RAHMAN ◽  
DAMANBHALANG RYNJAH ◽  
KAMALLOCHAN BARMAN ◽  
SARANGA SHEKHAR BORDOLOI ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Patient Compliance ◽  
Delivery System ◽  
Oral Drug Delivery ◽  
Antihypertensive Drugs ◽  
Polymeric Nanoparticles ◽  
Delivery Systems ◽  
Water Soluble ◽  
Oral Drug

Among various routes of drug delivery, Oral administration is the most convenient route because of its high patient compliance. Although oral drug delivery is effective for drugs with high aqueous solubility and epithelial permeability; however for poorly aqueous soluble drug the membrane permeability, chemical, and enzymatic stability of drugs are the major limitations in successful oral drug delivery. Almost 70% of the new drug candidates which shows poor bioavailability, the antihypertensive drugs are among those. Novel drug delivery systems are available in many areas to overcome the problems associated with hydrophobic drugs and the nanotechnology-based drug delivery system is the most potential to beat the challenges related to the oral route of administration with some important advantages such as the colloidal size, biocompatibility, lowered dose size, reduced toxicity, patient compliance and drug targeting. The foremost common nanotechnology-based strategies utilized in the development of delivery systems are nano-emulsions, nano-suspensions, dendrimers, micelles, liposomes, solid lipid nanoparticles, polymeric nanoparticles, carbon nanotubes, Self-Nano-emulsifying Drug Delivery System, proliposomes, nano-crystals, and so forth, which give controlled, sustained, and targeted drug delivery. The appliance of those systems within the treatment of hypertension continues to broaden. This review focuses on various nano-carriers available in oral drug administration for improving solubility profile, dissolution, and consequently bioavailability of hydrophobic antihypertensive drugs.

scholarly journals Self-Nano-Emulsifying Drug-Delivery Systems: From the Development to the Current Applications and Challenges in Oral Drug Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1194
Author(s):  
Aristote B. Buya ◽  
Ana Beloqui ◽  
Patrick B. Memvanga ◽  
Véronique Préat
Keyword(s):  
Drug Delivery ◽  
Patient Compliance ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Delivery Systems ◽  
Oral Drug ◽  
Statistical Design Of Experiments

Approximately one third of newly discovered drug molecules show insufficient water solubility and therefore low oral bio-availability. Self-nano-emulsifying drug-delivery systems (SNEDDSs) are one of the emerging strategies developed to tackle the issues associated with their oral delivery. SNEDDSs are composed of an oil phase, surfactant, and cosurfactant or cosolvent. SNEDDSs characteristics, their ability to dissolve a drug, and in vivo considerations are determinant factors in the choice of SNEDDSs excipients. A SNEDDS formulation can be optimized through phase diagram approach or statistical design of experiments. The characterization of SNEDDSs includes multiple orthogonal methods required to fully control SNEDDS manufacture, stability, and biological fate. Encapsulating a drug in SNEDDSs can lead to increased solubilization, stability in the gastro-intestinal tract, and absorption, resulting in enhanced bio-availability. The transformation of liquid SNEDDSs into solid dosage forms has been shown to increase the stability and patient compliance. Supersaturated, mucus-permeating, and targeted SNEDDSs can be developed to increase efficacy and patient compliance. Self-emulsification approach has been successful in oral drug delivery. The present review gives an insight of SNEDDSs for the oral administration of both lipophilic and hydrophilic compounds from the experimental bench to marketed products.

Fast Dissolution Electrospun Medicated Nanofibers for Effective Delivery of Poorly Water-Soluble Drugs

2021 ◽  
Vol 18 ◽  
Author(s):  
Yrysbaeva Aidana ◽  
Yibin Wang ◽  
Jie Li ◽  
Shuyue Chang ◽  
Ke Wang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Oral Drug Delivery ◽  
Drug Carriers ◽  
Water Soluble ◽  
Oral Drug ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Fast Dissolution

Background: Electrospinning is developing rapidly from an earlier laboratory method into an industrial process. The clinical applications are approached in various ways through electrospun medicated nanofibers. The fast-dissolving oral drug delivery system (DDS) among them is one of the most promising routes in the near future for commercial applications. Methods: Related papers are investigated, including the latest research results, on electrospun nanofiber-based fast-dissolution DDSs. Results: Several relative topics have been concluded: 1) the development of electrospinning, ranging from 1-fluid blending to multi-fluid process and potential applications in the formation of medicated nanofibers involving poorly water-soluble drugs; 2) Selection of appropriate polymer matrices and drug carriers for filament formation; 3) Types of poorly water-soluble drugs ideal for fast oral delivery; 4) The methods for evaluating fast-dissolving nanofibers; 5) The mechanisms that promote the fast dissolution of poorly water-soluble drugs by electrospun nanofibers; 6) the important issues for further development of electrospun medicated nanofibers as oral fast-dissolving drug delivery systems. Conclusions & Perspectives: The unique properties of electrospun-medicated nanofibers can be used as oral fast dissolving DDSs of poorly water-soluble drugs. However, some significant issues need to be investigated, such as scalable productions and solid dosage form conversions.

Design of a Soft, Self-Uncoiling Stent for Extended Retention of Drug Delivery in the Small Intestine

2020 ◽  
Author(s):  
Sunandita Sarker ◽  
Ryan Jones ◽  
Gabriel Chow ◽  
Benjamin Terry
Keyword(s):  
Drug Delivery ◽  
Small Intestine ◽  
Oral Drug Delivery ◽  
Ileocecal Valve ◽  
Drug Carriers ◽  
Oral Formulation ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Biological Drugs

Abstract Despite being the preferred route of drug administration, the oral formulation of biological drugs is limited due to its intrinsic instability, low permeability, and physical, chemical and immunological barriers. Various innovative swallowable technologies such as drug-loaded, dissolvable microneedles, mucoadhesive patches, and various microdevices present unique drug-carrying capabilities. The current work presents a novel soft stent platform that can facilitate contact between the small intestine tissue and drug carriers to enhance drug absorption and increase residence time. This study aims to prove the concept of this novel platform and determine if the soft stent will retain orally to the ileocecal valve longer than a capsule-shaped bolus. Benchtop studies on an intestinal simulator showed successful retention of the soft stent compared to a control capsule. In vivo studies in pig models also showed that the soft stent was retained longer than the control capsule. Overall, this study shows promise that this novel platform could be used for oral drug delivery of biologics.

scholarly journals Biomimetic insulin-imprinted polymer nanoparticles as a potential oral drug delivery system

2017 ◽  
Vol 67 (2) ◽  
pp. 149-168 ◽  
Author(s):  
Pijush Kumar Paul ◽  
Alongkot Treetong ◽  
Roongnapa Suedee
Keyword(s):  
Molecularly Imprinted Polymers ◽  
Oral Drug Delivery ◽  
Three Dimensional ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Functional Monomers ◽  
Oral Drug Delivery System ◽  
Nanosized Material ◽  
Glucose Reduction

AbstractIn this study, we investigate molecularly imprinted polymers (MIPs), which form a three-dimensional image of the region at and around the active binding sites of pharmaceutically active insulin or are analogous to b cells bound to insulin. This approach was employed to create a welldefined structure within the nanospace cavities that make up functional monomers by cross-linking. The obtained MIPs exhibited a high adsorption capacity for the target insulin, which showed a significantly higher release of insulin in solution at pH 7.4 than at pH 1.2. In vivo studies on diabetic Wistar rats showed that the fast onset within 2 h is similar to subcutaneous injection with a maximum at 4 h, giving an engaged function responsible for the duration of glucose reduction for up to 24 h. These MIPs, prepared as nanosized material, may open a new horizon for oral insulin delivery.

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