scholarly journals Engineering of Nanofibrous Amorphous and Crystalline Solid Dispersions for Oral Drug Delivery

Pharmaceutics ◽  
2018 ◽  
Vol 11 (1) ◽  
pp. 7 ◽  
Author(s):  
Laura Modica de Mohac ◽  
Alison Keating ◽  
Maria de Fátima Pina ◽  
Bahijja Raimi-Abraham
Keyword(s):  
Oral Drug Delivery ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Oral Drug ◽  
Crystalline Solid ◽  
Particle Size Reduction ◽  
Emerging Trends ◽  
Nano Crystalline ◽  
Water Soluble Drugs

Poor aqueous solubility (<0.1 mg/mL) affects a significant number of drugs currently on the market or under development. Several formulation strategies including salt formation, particle size reduction, and solid dispersion approaches have been employed with varied success. In this review, we focus primarily on the emerging trends in the generation of amorphous and micro/nano-crystalline solid dispersions using electrospinning to improve the dissolution rate and in turn the bioavailability of poorly water-soluble drugs. Electrospinning is a simple but versatile process that utilizes electrostatic forces to generate polymeric fibers and has been used for over 100 years to generate synthetic fibers. We discuss the various electrospinning studies and spinneret types that have been used to generate amorphous and crystalline solid dispersions.

Fast-dissolving Solid Dispersions for the Controlled Release of Poorly Water-soluble Drugs

2020 ◽  
Vol 26 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Beom-Jin Lee ◽  
Thao T.D. Tran
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Oral Drug Delivery ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Oral Drug ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

: Solid dispersions offer many advantages for oral drug delivery of poorly water-soluble drugs over other systems, including an increase in drug solubility and drug dissolution. The improvement of drug absorption and higher bioavailability of active pharmaceutical ingredients in the gastrointestinal tract have been reported in various studies. In certain circumstances, a rapid pharmacological effect is required for patients. Fast-dissolving solid dispersions provide an ideal formulation in such cases. This report will provide an overview of current studies on fast-dissolving solid dispersions, including not only solid dispersion powders with fast dissolution rates but also specific does forms for the controlled release of poorly water-soluble drugs. Specifically, the applications of fast-dissolving solid dispersions will be described in every specific case. Moreover, pharmaceutical approaches and the utilization of polymers will be summarized. The classification and analysis of fast-dissolving solid dispersions could provide insight into strategies and potential applications in future drug delivery developments.

scholarly journals Design and Characterization of Phosphatidylcholine-Based Solid Dispersions of Aprepitant for Enhanced Solubility and Dissolution

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 407
Author(s):  
Sooho Yeo ◽  
Jieun An ◽  
Changhee Park ◽  
Dohyun Kim ◽  
Jaehwi Lee
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Promising Alternative ◽  
Dispersion System ◽  
Enhanced Solubility ◽  
Water Soluble Drugs

This study aimed to improve the solubility and dissolution of aprepitant, a drug with poor aqueous solubility, using a phosphatidylcholine (PC)-based solid dispersion system. When fabricating the PC-based solid dispersion, we employed mesoporous microparticles, as an adsorbent, and disintegrants to improve the sticky nature of PC and dissolution of aprepitant, respectively. The solid dispersions were prepared by a solvent evaporation technique and characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry, and X-ray powder diffraction. The FTIR results showed that aprepitant interacted with the PC carrier by both hydrogen bonds and van der Waals forces that can also be observed in the interaction between aprepitant and polymer carriers. The solid dispersions fabricated with only PC were not sufficient to convert the crystallinity of aprepitant to an amorphous state, whereas the formulations that included adsorbent and disintegrant successfully changed that of aprepitant to an amorphous state. Both the solubility and dissolution of aprepitant were considerably enhanced in the PC-based solid dispersions containing adsorbent and disintegrant compared with those of pure aprepitant and polymer-based solid dispersions. Therefore, these results suggest that our PC-based solid dispersion system is a promising alternative to conventional formulations for poorly water-soluble drugs, such as aprepitant.

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.

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.

scholarly journals Nanotechnology Based Approaches for Enhancing Oral Bioavailability of Poorly Water Soluble Antihypertensive Drugs

Scientifica ◽  
2016 ◽  
Vol 2016 ◽  
pp. 1-11 ◽  
Author(s):  
Mayank Sharma ◽  
Rajesh Sharma ◽  
Dinesh Kumar Jain
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Antihypertensive Drugs ◽  
Aqueous Solubility ◽  
Oral Route ◽  
Water Soluble ◽  
Oral Drug ◽  
Convenient Route ◽  
Poorly Water Soluble ◽  
Novel Drug

Oral administration is the most convenient route among various routes of drug delivery as it offers high patient compliance. However, the poor aqueous solubility and poor enzymatic/metabolic stability of drugs are major limitations in successful oral drug delivery. There are several approaches to improve problems related to hydrophobic drugs. Among various approaches, nanotechnology based drug delivery system has potential to overcome the challenges associated with the oral route of administration. Novel drug delivery systems are available in many areas of medicine. The application of these systems in the treatment of hypertension continues to broaden. The present review focuses on various nanocarriers available in oral drug administration for improving solubility profile, dissolution, and consequently bioavailability of hydrophobic antihypertensive drugs.

scholarly journals A Novel Rheological Method to Assess Drug-Polymer Interactions Regarding Miscibility and Crystallization of Drug in Amorphous Solid Dispersions for Oral Drug Delivery

Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 625 ◽  
Author(s):  
Georgia Tsakiridou ◽  
Christos Reppas ◽  
Martin Kuentz ◽  
Lida Kalantzi
Keyword(s):  
In Silico ◽  
Oral Drug Delivery ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Water Soluble ◽  
Oral Drug ◽  
Main Task ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Polymer Interactions

Solid dispersions provide a key technology to formulate poorly water-soluble drugs, and a main task of early development is appropriate selection of polymer. This study investigates the use of a novel rheology-based approach to evaluate miscibility and interactions of drugs with polymers regarding amorphous solid drug dispersions for oral administration. Tacrolimus was used as model drug and hydroxypropyl cellulose, ethylcellulose, Soluplus®, polyethyleneglycol 6000, Poloxamer-188 (Koliphor-188), and Eudragit® S100 were used as excipients. Solvent-based evaporation methods were used to prepare binary solid dispersions of drug and polymer. Data of the dilute solution viscosimetry were compared with in silico calculations of the Hansen solubility parameter (HSP), as well as phase separation/crystallization data obtained from X-ray diffraction and differential scanning calorimetry. HSP calculations in some cases led to false positive predictions of tacrolimus miscibility with the tested polymers. The novel rheology-based method provided valuable insights into drug-polymer interactions and likely miscibility with polymer. It is a rather fast, inexpensive, and robust analytical approach, which could be used complementary to in silico-based evaluation of polymers in early formulation development, especially in cases of rather large active pharmaceutical ingredients.

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.

scholarly journals An Overview on the Recent Technologies and Advances in Drug Delivery of Poorly Water-Soluble Drugs

2019 ◽  
pp. 180-195
Keyword(s):  
Crystal Engineering ◽  
General Circulation ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Phase System ◽  
Particle Size Reduction ◽  
Pharmaceutical Ingredients ◽  
Solubility Improvement ◽  
New Chemical Entities ◽  
Water Soluble Drugs

Solubility can be defined as the amount of solute dissolved in a solvent at certain conditions to yield a single-phase system. Solubility of active pharmaceutical ingredients is considered the main parameter to get the most desired drug concentration in general circulation in order to achieve the desired therapeutic effect. Poor aqueous solubility considered the main problem occurs in the formulation progress of new chemical entities; in addition to the standard improvement; solubility is the main dispute for formulation scientists. The drug must appear as solution at the site of absorption in order to be absorbed. Many physical or chemical modification techniques are used to improve the solubility of low aqueous soluble drugs, in addition to other techniques such as particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant and complexation. The selection of the solubility improvement methods depends on drug characteristics, location of absorption and the features of the administered dosage form.

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