A COMPARATIVE ASSESSMENT OF VESICULAR FORMULATIONS: TRANSFERSOMES AND CONVENTIONAL LIPOSOMES LOADED IVABRADINE HYDROCHLORIDE (original) (raw)

Novel Vesicular Drug Carriers for Bioavailability Enhancement

The objective of the study is to evaluate the potential of novel vesicular drug carriers for bioavailability enhancement. Novel vesicular drug delivery carriers intend to deliver the drug at a rate directed by need of body during the period of treatment, and channel the active entity to the site of action. Encapsulation of drug in vesicular structures prolongs the existence of drug in systemic circulation and reduces the toxicity, if selective uptake can be achieved. Vesicular drug delivery systems have been used to improve the therapeutic index, solubility, stability and rapid degradation of drug molecule. This system reduces the cost of therapy by bioavailability improvement of medication, especially in case of poorly soluble drugs. Thus a number of novel vesicular drug delivery systems have been developed that enhance the bioavailability and provide sustained or controlled release of drug. The focus of this review is to discuss various lipoidal and non-lipoidal vesicles with special emphasis on the bioavailability enhancement of drugs.

Lipid vesicles: applications, principal components and methods used in their formulations: A review

Acta Biológica Colombiana

Liposomes and niosomes are currently the most studied lipid vesicles in the nanomedicine field. The system formed by a phospholipid bilayer in aqueous medium allows these vesicles to carry both hydrophilic and lipophilic compounds, providing an increase in solubility of drugs lready used in conventional therapy. The focus on the development of these vesicles should be directed to determining the ideal composition, with low toxicity, biocompatibility and which remains stable for long periods. These characteristics are related to the components used for formulation and the substances that will be encapsulated. Another important point relates to the methods used during formulation, which are important in determining the type of vesicle formed, whether these be large or small, unilamellar or multilamellar. Because of the deliberate actions applied in the development of these vesicles, this review sought to gather updated information regarding the different methods used, including their ...

In vitro Characterization and Release Studies of Combined Nonionic Surfactant-Based Vesicles for the Prolonged Delivery of an Immunosuppressant Model Drug

International Journal of Nanomedicine

Background: Cyclosporine A (CsA) is an exceptional immunosuppressant used for the treatment of immune disorders. Niosomal vesicles are promising drug carriers that are formed by self-association of nonionic surfactants and cholesterol in an aqueous phase. The objective of the study was to formulate combined nonionic surfactant based vesicles and to evaluate their in vitro characterization, release studies and in vivo studies. Materials and Methods: Five niosomal formulations (F 7 to F 11) were prepared using the thin film hydration method. The molar ratio of cholesterol and non-ionic surfactant taken was 1:1. In formulation F 10 , the combination of surfactants Span 20 and Brij 35 was used. The niosomes were characterized by zeta sizer and SEM for particle size analysis, in vitro drug release and stability studies. The pharmacokinetic studies were conducted on healthy albino rabbits. Results: The size of niosome was found in the range of 427.1 nm to 972.3 nm. SEM image of optimized formulations F 10 exhibit the spherical nature of niosomal vesicles. DSC thermograms of niosomal formulations exhibited a broadened endothermic peak. The stability study exhibited that all formulations are stable and negligible change of vesicle size and entrapment was observed with time. The percentage drug release was significantly higher as compared to CsA plain dispersion for all niosomal formulations at pH 1.2 and 7.4. The release kinetic behavior showed that all preparations were best described by zero order and can release active ingredient in a sustained manner. The pharmacokinetic data showed the test formulation (F10) possessed greater bioavailability as compared to the reference formulation (CsA aqueous dispersion). Conclusion: The formulation F 10 demonstrated a comparatively more delayed rate of release with enhanced dissolution as compared to a single surfactant scheme. The F 10 formulation can be a remarkable nanotechnology for prolonged delivery of CsA orally with improved dissolution profile and bioavailability.

Novel Approaches in vesicular drug delivery systems

2013

Vesicular drug delivery system is one of the most promising particulate Drug carrier systems in the large family of pharmaceutical nanocarriers. Drug carriers are substances that serve as mechanisms to improve the delivery and effectiveness of drugs to the target sites of pharmacological actions. The application of vesicular system in drug delivery has changed the definitions of diagnosis and treatment in different aspects of biomedical field. Vesicular system is used as vehicle for wide variety of drugs, vaccines, enzymes, and genetic materials and now for some nutritional supplements as well. This review will focus on need for development of Vesicular system as there are some major drawbacks in present conventional dosage forms and Liposomal dosage form and its different modified forms, which are the most successful vesicular system.

Formulation and Evaluation of Transferosomes Loaded with an Anti-Hyperlipidemic Drug

Journal of Scientific Research and Reports, 2021

The primary goal of this research is to create transferosome formulations that contain an anti-hyperlipidemic medication. Simvastatin, the medication employed in the formulation, has a low bioavailability of 60% and undergoes substantial hepatic degradation. These are the deformable nano-vesicles which can deliver both hydrophilic and hydrophobic drugs through transdermal route to enhance the Bioavailability of drugs which undergoes extensive hepatic metabolism when given through oral route which can increase patient compliance. Transferosomes are prepared and characterized by various evaluation tests like SEM analysis, vesicular size, surface morphology. After all evaluations done, Out of 12 formulations F2 formulation showed more entrapment efficiency. The reason for this is that there are more phospholipids present, and as the surfactant concentration rises, medication release becomes more rapid. Our main goal is to improve bioavailability, which can be accomplished by optimis...

The New Era of Vesicular Drug Delivery System: A Review

IJIRT, 2021

The article provides an up-to-date review of several vesicular drug delivery systems, which are designed to administer drugs at a controlled pace determined by the body's needs. Vesicular drug delivery systems are primarily utilized for medication targeting by localizing the drug action in the sick or inflamed tissue, location, or organ of action through the use of various pharmaceutical carriers. Novel Vesicular drug administration has been employed to improve the therapeutic index, solubility, and speed of drug breakdown. This vesicular system prolongs the presence of the drug in the circulatory system by releasing the drug in a controlled manner, as well as reducing the drug's toxicity. Thus, a variety of vesicular systems, such as Niosomes, Liposomes, Transferosomes, Ethosomes, Aquasomes, Cubosomes, and Ufasomes, have been designed to improve the potential of new therapeutic compounds by encapsulating an active ingredient within the vesicular structure of a system. To offer the drug in the form of a novel drug delivery system, several carriers such as polymeric micelles or vesicular systems, particulate systems or colloidal carrier systems, and macro and micromolecules are used. In this study, we will focus on various forms of novel vesicular systems in terms of their types, advantages, shortcomings, possibilities of vesicular drug delivery system in gel form, and recent applications. In this study, we will focus on many forms of innovative vesicular systems in terms of their types, benefits, drawbacks, possibilities of vesicular drug delivery system in gel form, and recent applications in Pharmaceutical sciences.

Elastic Vesicles for Transdermal Drug Delivery of Hydrophilic Drugs: A Comparison of Important Physicochemical Characteristics of Different Vesicle Types

Journal of Biomedical Nanotechnology, 2012

The aim of this study is to evaluate the influence of different lipid vesicular systems on the skin permeation abilityof hydrophilic molecules, and understand if and which vesicle physicochemical properties may be used as predictive tools. Calcein and carboxyfluorescein were used as hydrophilic drug models. All vesicles (conventional liposomes [CLs], transfersomes [TRs] and invasomes [INVs], were characterized for particle size distribution, -potential, vesicular shape and morphology, encapsulation efficiency, integrity, colloidal stability, elasticity and finally in vitro human skin permeation. Dynamic light scattering (DLS) and cryo-transmission electron microscopy (cryo-TEM) defined that almost all vesicles had spherical structure, low polydispersity (PI < 0 2) and nanosize. Elasticity values (measured by extrusion through membranes) were in the order INVs > TRs > CLs. Three vesicle types were selected (having different elasticity) and in vitro skin permeation experiments demonstrated thatcalcein permeation was minimal from an aqueous solution, slightly enhanced from CLs, and enhanced by 1.8 and 7.2 times from TRs and INVs, respectively. Permeation and elasticity values were correlated by rank order but not linearly, indicating that elasticity can be used as a crude predictive tool for enhancement of skin transport. Drug encapsulation efficiency was not found to be an important factor in the current study.

Vesicular Drug Delivery System -An Over View

The application of vesicular system in drug delivery has changed the definitions of diagnosis and treatment in different aspects of biomedical field. The vesicular system as liposome's, niosomes, sphinosomes, transferosomes, pharmacosomes and ufasomes are used to improve the new drug molecules by encapsulating an active medicament inside vesicular structure in one such system. It prolongs the existence of the drug in systemic circulation and finally reduces the toxicity. Such different systems are widely used in gene delivery, tumor targeting to brain, oral formulations, in stability and permeability problems of drugs. In this review we really focused on different aspects of vesicular system in terms of its advantages, limitation, applications and different marketed product of vesicular system as novel drug delivery.

Liposome formulation of poorly water soluble drugs: optimisation of drug loading and ESEM analysis of stability

International journal of pharmaceutics, 2004

Liposomes due to their biphasic characteristic and diversity in design, composition and construction, offer a dynamic and adaptable technology for enhancing drug solubility. Starting with equimolar egg-phosphatidylcholine (PC)/cholesterol liposomes, the influence of the liposomal composition and surface charge on the incorporation and retention of a model poorly water soluble drug, ibuprofen was investigated. Both the incorporation and the release of ibuprofen were influenced by the lipid composition of the multi-lamellar vesicles (MLV) with inclusion of the long alkyl chain lipid (dilignoceroyl phosphatidylcholine (C24PC)) resulting in enhanced ibuprofen incorporation efficiency and retention. The cholesterol content of the liposome bilayer was also shown to influence ibuprofen incorporation with maximum ibuprofen incorporation efficiency achieved when 4 micromol of cholesterol was present in the MLV formulation. Addition of anionic lipid dicetylphosphate (DCP) reduced ibuprofen dr...

Development and Characterization of Liposome‐Based Formulation of Amiloride Hydrochloride

Journal of Dispersion Science and Technology, 2008

This paper focuses on the preparation and characterization of new, stable phospholipid formulations as carriers for dermal delivery of diclofenac (DCF). To prepare these vesicles two water miscible permeation enhancers (PE) with glycol group: diethyleneglycol monoethyl ether (Transcutol ® , Trc) and propylene glycol (PG), were added at different concentrations (10%, 20%, 30%, 40%, 50%) during the preparation of diclofenac loaded soy lecithin (SL) liposomes. We added Transcutol ® or propylene glycol to the hydrophilic phase in order to obtain new systems able to enhance the skin delivery of diclofenac thanks to the synergic effect of glycols and phospholipids. Permeation enhancing vesicles (PEVs) were characterised by means of transmission electron microscopy (TEM), zeta potential, entrapment efficiency (E%) and reological properties. TEM micrographies showed that vesicle morphology was irregular and an ovoidal shape was predominant. Vesicular size decreased in the presence of Transcutol ® (up to 20%) and propylene glycol (from 10% to 50%). E% increased in vesicles prepared with 10% and 20% of Trc with respect to SL liposomes and PEVs containing the same amount of PG. Vesicle dispersions were slowly frozen and unfrozen to break the vesicle bilayer and the rheological measurements of defrosted samples were carried out without stirring to avoid vesicle reconstitution. The shear stress values were measured for a given rate of shear. Results showed that the presence of Trc or PG in vesicle dispersions facilitated the vesicle segregation from lamellar phase allowing a reduction of hysteresis loop area and apparent viscosity.