scholarly journals The effect of drug ionization on lipid-lased formulations for the oral delivery of anti-psychotics

ADMET & DMPK ◽  
2020 ◽  
Author(s):  
Tahlia R Meola ◽  
Kara Paxton ◽  
Paul Joyce ◽  
Hayley B Schultz ◽  
Clive A Prestidge
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Fold Increase ◽  
Water Soluble ◽  
Equilibrium Solubility ◽  
Poorly Water Soluble Drugs ◽  
Physiochemical Properties ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Rate Limiting

<p class="ADMETabstracttext">Lipid-based formulations (LBFs) are well-known to improve the oral bioavailability of poorly water-soluble drugs (PWSDs) by presenting the drug to the gastrointestinal environment in a molecularly dispersed state, thus avoiding the rate-limiting dissolution step. Risperidone and lurasidone are antipsychotics drugs which experience erratic and variable absorption, leading to a low oral bioavailability. The aim of this research was to develop and investigate the performance of risperidone and lurasidone when formulated as an emulsion and silica-lipid hybrid (SLH). Lurasidone and risperidone were dissolved in Capmul® MCM at 100% and 80% their equilibrium solubility, respectively, prior to forming a sub-micron emulsion. SLH microparticles were fabricated by spray-drying a silica stabilised sub-micron emulsion to form a solid powder. The performances of the formulations were evaluated in simulated intestinal media under digesting conditions, where the emulsion and SLH provided a 17-fold and 23-fold increase in LUR solubilisation, respectively. However, the performance of RIS was reduced by 2.2-fold when encapsulated within SLH compared to pure drug. Owing to its pKa, RIS adsorbed to the silica and thus, dissolution was significantly hindered. The results reveal that LBFs may not overcome the challenges of all PWSDs and physiochemical properties must be carefully considered when predicting drug performance.</p>

Development of biodegradable porous starch foam for improving oral delivery of poorly water soluble drugs

2011 ◽  
Vol 403 (1-2) ◽  
pp. 162-169 ◽  
Author(s):  
Chao Wu ◽  
Zhongyan Wang ◽  
Zhuangzhi Zhi ◽  
Tongying Jiang ◽  
Jinghai Zhang ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

scholarly journals Polymeric Micelles, a Promising Drug Delivery System to Enhance Bioavailability of Poorly Water-Soluble Drugs

2013 ◽  
Vol 2013 ◽  
pp. 1-15 ◽  
Author(s):  
Wei Xu ◽  
Peixue Ling ◽  
Tianmin Zhang
Keyword(s):  
Drug Delivery ◽  
Residence Time ◽  
Oral Delivery ◽  
Polymeric Micelles ◽  
Water Soluble ◽  
Gi Tract ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Accepted Form

Oral administration is the most commonly used and readily accepted form of drug delivery; however, it is find that many drugs are difficult to attain enough bioavailability when administered via this route. Polymeric micelles (PMs) can overcome some limitations of the oral delivery acting as carriers able to enhance drug absorption, by providing (1) protection of the loaded drug from the harsh environment of the GI tract, (2) release of the drug in a controlled manner at target sites, (3) prolongation of the residence time in the gut by mucoadhesion, and (4) inhibition of efflux pumps to improve the drug accumulation. To explain the mechanisms for enhancement of oral bioavailability, we discussed the special stability of PMs, the controlled release properties of pH-sensitive PMs, the prolongation of residence time with mucoadhesive PMs, and the P-gp inhibitors commonly used in PMs, respectively. The primary purpose of this paper is to illustrate the potential of PMs for delivery of poorly water-soluble drugs with bioavailability being well maintained.

scholarly journals SOLID DISPERSIONS: RESUSCITATING ORAL DELIVERY OF HYDROPHOBIC DRUGS

2019 ◽  
pp. 213-217
Author(s):  
RUCHI AGRAWAL ◽  
ABID RAZA ◽  
OM PRAKASH PATEL
Keyword(s):  
Oral Delivery ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Future Trends ◽  
Hydrophobic Drugs ◽  
Poorly Water Soluble Drugs ◽  
Advantages And Disadvantages ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Viable Method

Objective: This review article explores solid dispersions (SDs) as one of the suitable approaches to formulate poorly water-soluble drugs. The objective of this review on SD techniques is to explore their utility as a feasible, simple, and economically viable method for augmentation of dissolution of hydrophobic drugs. Methods: Various types of SDs are classified and compared. Use of surfactants to stabilize the SDs and their potential advantages and disadvantages has been discussed. Different techniques for preparing and evaluating SDs are appraised along with discussions on scalability and industrial production. Review of the current research on SD along with future trends is also offered. Results: Based on the various researches, SDs offer an efficient means of improving bioavailability while concurrently contributing to lower toxicity and dose-reduction. Conclusion: Solid-dispersions have been and continue to be one of the key technologies for solving the issue of poor solubility for newer hydrophobic molecules which are being discovered. This would give a new lease of life for such drugs enabling them to be delivered in an effective way.

Nanoporous silicon to enhance oral delivery of poorly water-soluble drugs

2021 ◽  
pp. 399-426
Author(s):  
H.B. Schultz ◽  
P. Joyce ◽  
C.A. Prestidge ◽  
T.J. Barnes
Keyword(s):  
Oral Delivery ◽  
Water Soluble ◽  
Nanoporous Silicon ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Potentials of proniosomes for improving the oral bioavailability of poorly water-soluble drugs

2013 ◽  
Vol 41 (1) ◽  
pp. 51-62 ◽  
Author(s):  
Shuangshuang Song ◽  
Baocheng Tian ◽  
Fen Chen ◽  
Wenji Zhang ◽  
Yusheng Pan ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

A liposome-micelle-hybrid (LMH) oral delivery system for poorly water-soluble drugs: Enhancing solubilisation and intestinal transport

2020 ◽  
Vol 154 ◽  
pp. 338-347 ◽  
Author(s):  
Bilquis Romana ◽  
Md. Musfizur Hassan ◽  
Fabio Sonvico ◽  
Gabriela Garrastazu Pereira ◽  
Alex F. Mason ◽  
...  
Keyword(s):  
Delivery System ◽  
Oral Delivery ◽  
Intestinal Transport ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Oral Delivery System ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble
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