Pharmacosomes: An approach to improve biopharmaceutical properties of drugs basic considerations in development

Author(s):  
Popat Kumbhar ◽  
Tejaswini Shinde ◽  
Tejaswini Jadhav ◽  
Tejas Gavade ◽  
Rushikesh Sorate ◽  
...  

Vesicular drug delivery systems including niososmes, liposomes, pharmacosomes, transferosomes, electrosomes, ethosomes, etc have been widely accepted for controlled delivery of the drug. Amongst, all these drug delivery systems pharmacosomes are gaining more attention of the researchers due to several benefits such as high entrapment efficiency, improved biopharmaceutical properties, and pharmacokinetic performance, no leakage or loss of drug, stability, etc. Pharmacosomes are amphiphilic phospholipid complexes of drugs having active hydrogen that bind to phospholipids and self-assembled into vesicles in an aqueous medium. Both hydrophilic and lipophilic drugs have been formulated into pharmacosomes that caused improved solubility and permeability of drugs. Pharmacosomes are prepared by using various techniques such as hand shaking method, ether injection, solvent evaporation method, supercritical fluid approach, etc and are characterized for prodrug confirmation, surface morphology, crystal state measurement, in vitro drug release, and stability, etc. Despite wide research and highly encouraging results in the preclinical studies, translation of these nanomedicines from laboratory to market has been very limited. The main aim of this review is to describe comprehensively the potential of pharmacosomes as a vesicular drug delivery system focusing mainly on their conventional and advanced methods of preparation, different characterization techniques, and their applications in the delivery of different types of drugs with improved biopharmaceutical properties and pharmacokinetic performance.

2019 ◽  
Vol 9 (1) ◽  
pp. 279-285 ◽  
Author(s):  
Priyanka Chaurasiya ◽  
Eisha Ganju ◽  
Neeraj Upmanyu ◽  
Sudhir Kumar Ray ◽  
Prabhat Jain

Novel drug delivery systems are now a days is creating a new interest in development of drug deliveries. Vesicular drug delivery system is also a part of these novel drug delivery systems. TDDS is the permeability of the skin, it is permeable to small molecules, lipophilic drug and highly impermeable to the macromolecules and hydrophilic drugs. Recent approaches have resulted in design of two vesicular carriers, ethosomes and ultra flexible lipid based elastic vesicles, transferosomes. Transferosomes have recently been introduced, which are capable of transdermal delivery of low as well as high molecular weight drugs. This offers several potential advantages over conventional routes like avoidance of first pass metabolism, predictable and extended duration of activity, minimizing undesirable side effects, utility of short half life drugs, improving physiological and pharmacological response and have been applied to increases the efficiency of the material transfer across the intact skin, by the use of penetration enhancers, iontophoresis, sonophoresis and use of colloidal carriers such as lipid vesicles (liposomes & proliposomes) and non-ionic surfactant vesicles (niosomes & proniosomes). It is suitable for controlled and targeted drug delivery and it can accommodate drug molecules with wide range of solubility. Due to its high deformability it gives better penetration of intact vesicles. They are biocompatible and biodegradable as they are made from natural phospholipids and have high entrapment efficiency. The preparation variables are depending upon the procedure involved for manufacturing of formulation and the preparation procedure was accordingly optimized and validated. Characterization of transferosomes can be done to know the vesicle size, morphology, drug content, entrapment efficiency, penetration ability, occlusion effect, surface charge, in vitro drug release, in vitro skin penetration etc., It increases stability of labile drugs and provides control release. Transferosomes thus differs from such more conventional vesicles primarily by its softer, more deformable, better adjustable artificial membrane. Keywords: Novel Drug Delivery System, Biocompatible, Characterization, Transferosomes.


Author(s):  
Anamika Saxena Saxena ◽  
Santosh Kitawat ◽  
Kalpesh Gaur ◽  
Virendra Singh

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 725
Author(s):  
Yuseon Shin ◽  
Patihul Husni ◽  
Kioh Kang ◽  
Dayoon Lee ◽  
Sehwa Lee ◽  
...  

The combination of nanotechnology and chemotherapy has resulted in more effective drug design via the development of nanomaterial-based drug delivery systems (DDSs) for tumor targeting. Stimulus-responsive DDSs in response to internal or external signals can offer precisely controlled delivery of preloaded therapeutics. Among the various DDSs, the photo-triggered system improves the efficacy and safety of treatment through spatiotemporal manipulation of light. Additionally, pH-induced delivery is one of the most widely studied strategies for targeting the acidic micro-environment of solid tumors. Accordingly, in this review, we discuss representative strategies for designing DDSs using light as an exogenous signal or pH as an endogenous trigger.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 861
Author(s):  
Jacopo Cardellini ◽  
Arianna Balestri ◽  
Costanza Montis ◽  
Debora Berti

In the past decade(s), fluorescence microscopy and laser scanning confocal microscopy (LSCM) have been widely employed to investigate biological and biomimetic systems for pharmaceutical applications, to determine the localization of drugs in tissues or entire organisms or the extent of their cellular uptake (in vitro). However, the diffraction limit of light, which limits the resolution to hundreds of nanometers, has for long time restricted the extent and quality of information and insight achievable through these techniques. The advent of super-resolution microscopic techniques, recognized with the 2014 Nobel prize in Chemistry, revolutionized the field thanks to the possibility to achieve nanometric resolution, i.e., the typical scale length of chemical and biological phenomena. Since then, fluorescence microscopy-related techniques have acquired renewed interest for the scientific community, both from the perspective of instrument/techniques development and from the perspective of the advanced scientific applications. In this contribution we will review the application of these techniques to the field of drug delivery, discussing how the latest advancements of static and dynamic methodologies have tremendously expanded the experimental opportunities for the characterization of drug delivery systems and for the understanding of their behaviour in biologically relevant environments.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1108
Author(s):  
Oana Craciunescu ◽  
Madalina Icriverzi ◽  
Paula Ecaterina Florian ◽  
Anca Roseanu ◽  
Mihaela Trif

Osteoarthritis (OA) is a degenerative joint disease. An objective of the nanomedicine and drug delivery systems field is to design suitable pharmaceutical nanocarriers with controllable properties for drug delivery and site-specific targeting, in order to achieve greater efficacy and minimal toxicity, compared to the conventional drugs. The aim of this review is to present recent data on natural bioactive compounds with anti-inflammatory properties and efficacy in the treatment of OA, their formulation in lipid nanostructured carriers, mainly liposomes, as controlled release systems and the possibility to be intra-articularly (IA) administered. The literature regarding glycosaminoglycans, proteins, polyphenols and their ability to modify the cell response and mechanisms of action in different models of inflammation are reviewed. The advantages and limits of using lipid nanoformulations as drug delivery systems in OA treatment and the suitable route of administration are also discussed. Liposomes containing glycosaminoglycans presented good biocompatibility, lack of immune system activation, targeted delivery of bioactive compounds to the site of action, protection and efficiency of the encapsulated material, and prolonged duration of action, being highly recommended as controlled delivery systems in OA therapy through IA administration. Lipid nanoformulations of polyphenols were tested both in vivo and in vitro models that mimic OA conditions after IA or other routes of administration, recommending their clinical application.


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