Vesicular Drug Delivery Systems Research Articles

Novel Vesicular Bilosomal Delivery Systems for Dermal/Transdermal Applications.

The application of therapeutically active molecules through the dermal/transdermal route into the skin has evolved as an attractive formulation strategy in comparison to oral delivery systems for the treatment of various disease conditions. However, the delivery of drugs across the skin is limited due to poor permeability. Dermal/transdermal delivery is associated with ease of accessibility, enhanced safety, better patient compliance, and reduced variability in plasma drug concentrations. It has the ability to bypass the first-pass metabolism, which ultimately results in steady and sustained drug levels in the systemic circulation. Vesicular drug delivery systems, including bilosomes, have gained significant interest due to their colloidal nature, improved drug solubility, absorption, and bioavailability with prolonged circulation time for a large number of new drug molecules. Bilosomes are novel lipid vesicular nanocarriers comprising bile salts, such as deoxycholic acid, sodium cholate, deoxycholate, taurocholate, glycocholate or sorbitan tristearate. These bilosomes are associated with high flexibility, deformability, and elasticity attributed to their bile acid component. These carriers are advantageous in terms of improved skin permeation, increased dermal and epidermal drug concentration, and enhanced local action with reduced systemic absorption of the drug, resulting in reduced side effects. The present article provides a comprehensive overview of the biopharmaceutical aspects of dermal/transdermal bilosome delivery systems, their composition, formulation techniques, characterization methods, and applications.

Innovative approaches in characterizing and developing methods for lipoidal vesicular drug delivery systems

Lipoidal vesicular systems, including liposomes, ethosomes, and transferosomes, represent a significant advancement in targeted drug delivery, offering enhanced bioavailability, controlled release, and specific targeting capabilities. This review discusses the types of lipoidal vesicular systems, their methods of characterization, method development, applications, advantages, challenges, and future perspectives. These systems have shown immense potential in diverse therapeutic areas, including cancer therapy, infectious diseases, gene therapy, and transdermal drug delivery. Despite the challenges in stability, scalability, and targeting, ongoing research and technological advancements promise to expand their applications and improve therapeutic outcomes.

Molecular docking, molecular dynamics simulation, preparation, and characterization of naltrexone-phospholipid complex: A novel cargo with improved loading into multivesicular liposomes

Naltrexone hydrochloride (NTX), a water-soluble opioid receptor antagonist, is prescribed widely for opioid and alcohol dependence and pain reduction. However, the significant limitations of NTX are low lipophilicity and extensive first-pass metabolism. This study aimed to design and prepare a novel phospholipid complex of NTX and load it into multivesicular liposomes (MVLs). In silico studies, including molecular docking and molecular dynamics (MD) simulation, were performed to determine the interactions between NTX and phospholipid and evaluate their best molar ratio to prepare the complex, respectively. The NTX phospholipid complex was prepared by solvent evaporation technique and characterized by PXRD, SEM, FTIR, 1HNMR, solubility study, and n-octanol/water partition coefficient analyses. NTX-SPC complex-loaded MVLs (NTX-SPC-MVLs) were prepared by the double-emulsion method and characterized by encapsulation efficiency (EE)%, size, PXRD, FTIR, SEM, and release pattern. MD simulation reported the 1:1.5 M ratio of NTX to phospholipid as the best molar ratio. Complexation led to reduced water solubility and enhanced n-octanol/water partition coefficient. Loading of NTX-SPC complex into MVLs enhanced EE and extended the release duration in comparison to NTX MVLs. Thus, the NTX-SPC complex may be an appropriate system to enhance the physicochemical features of NTX and improve the EE in vesicular drug delivery systems like MVLs.

Vesicular Drug Delivery Systems: Promising Approaches in Ocular Drug Delivery.

Ocular drug delivery poses unique challenges due to the complex anatomical and physiological barriers of the eye. Conventional dosage forms often fail to achieve optimal therapeutic outcomes due to poor bioavailability, short retention time, and off-target effects. In recent years, vesicular drug delivery systems have emerged as promising solutions to address these challenges. Vesicular systems, such as liposome, niosome, ethosome, transfersome, and others (bilosome, transethosome, cubosome, proniosome, chitosome, terpesome, phytosome, discome, and spanlastics), offer several advantages for ocular drug delivery. These include improved drug bioavailability, prolonged retention time on the ocular surface, reduced systemic side effects, and protection of drugs from enzymatic degradation and dilution by tears. Moreover, vesicular formulations can be engineered for targeted delivery to specific ocular tissues or cells, enhancing therapeutic efficacy while minimizing off-target effects. They also enable the encapsulation of a wide range of drug molecules, including hydrophilic, hydrophobic, and macromolecular drugs, and the possibility of combination therapy by facilitating the co-delivery of multiple drugs. This review examines vesicular drug delivery systems, their advantages over conventional drug delivery systems, production techniques, and their applications in management of ocular diseases.

Exploring the Therapeutic Potential of Vesicular Nanocarrier Systems for Elimination of Skin Cancer

Background:: Skin cancer, a common malignancy worldwide, has increased incidence and mortality. Thus, it is a public health issue and a significant illness burden, which increases treatment costs. Chemotherapy and surgery are used to treat skin cancer. However, conventional skin cancer treatments have several limitations, demanding the development of innovative, safe, and effective methods. To overcome these limitations of conventional topical dosage forms, many nanocarriers have been developed and tested for the targeted delivery of anticancer drugs. Objective:: The main objective of the present review was to discuss the utility of various vesicular nanocarrier systems to deliver anticancer drugs following topical administration to treat skin cancer. Methods:: For this review article, we scoured the scholarly literature using Science Direct, Google Scholar, and Pubmed. Discussion:: The vesicular drug delivery system has been intensively explored and developed as an alternative to conventional skin cancer drug delivery systems, especially for melanoma. They improve the penetration of anticancer drugs via the skin, reaching the cancer area with enough and killing cancer cells. Vesicles minimize skin irritation and drug degradation. This improves therapy efficacy and reduces systemic toxicity. Conclusion:: Utilizing the vesicular drug delivery system shows promise in treating skin cancer. Therefore, further research and inquiries are necessary to explore the therapeutic potential of these substances in treating skin cancer, intending to develop a personalized, efficient, and secure therapy approach for patients with this condition.

Liposome as a Potential Drug Delivery System in Addressing Skin Diseases: A Review

Abstract: It was asserted that the manufacturing of liposomes, which was first disclosed in 1961, was a useful technology for drug encapsulation. Furthermore, there are several cosmetic items on the market now that include liposomes. The liposomes are novel drug carrier systems due to their similarity in lipid composition with the epidermal membrane. As a result, they penetrate the epidermis to a greater extent, showing enhanced skin absorption and increased effectiveness of the encapsulated drug molecule. This review briefly addresses the skin's anatomy, skin conditions, and the topical delivery of drugs for the treatment of skin diseases with emphasis on psoriasis by utilizing liposomes and other vesicular drug delivery systems along with challenges and opportunities in the treatment of skin diseases. When compared to alternative distribution methods, their resemblance to biological membranes enables entry into the epidermal barrier. Liposomes are good at penetrating the skin more deeply and reducing therapeutic side effects, which offers hope for the successful treatment of skin problems. Applying liposomes topically has several benefits, including better skin bioavailability and targeting, increased skin hydration by surface adhesiveness, protection of skin structure from external stress, and prolonged dermal release. Further, they have got potential to target the encapsulated drug molecule into pilosebaceous structure, making them an ideal candidate for the treatment of hair follicles and sebaceous gland disorder.

Functionalized and theranostic lipidic and tocosomal drug delivery systems: potentials and limitations in cancer photodynamic therapy

Photodynamic therapy (PDT) is a multidisciplinary area, which involves photophysics and photochemical sciences and plays an important role in cancer diagnosis and treatment. PDT involves a photo-activable drug called photosensitizer (PS), a specific wavelength of light and cellular compounds to produce toxic oxygen species in a much-localized way to destroy malignant tumors. Despite the various benefits of PDT, some PS-related limitations hinder its use as an ideal treatment option for cancer. To address these limitations (e.g., poor bioavailability, weak permeability, hydrophobicity, and aggregation), lipid-based and vesicular drug delivery systems have been employed. These carrier systems possess the ability to enhance the bioavailability, permeability, and solubility of the drug. Furthermore, they tend to load hydrophobic and lipophilic compounds and can be employed for an efficient and targeted drug delivery. The purpose of this review is to highlight the precise idea of PDT, the limitations of PDT related to PS, and the application of lipidic and tocosomal carriers in PDT for the treatment of various types of cancers. Liposomes, nanoliposomes, solid lipid nanoparticles, vesicular phospholipid gels, exosomes, transferosomes, and tocosomes are presented as commonly–employed vesicular drug carriers. Moreover, the amalgamation of cell-based drug delivery systems (CBDDS) with PDT holds considerable potential as an encouraging avenue in cancer treatment, especially in the context of immunotherapy.

Recent Excavation of Nanoethosomes in Current Drug Delivery.

In the current era, the Transdermal delivery of bioactive molecules has become an area of research interest. The transdermal route of administration enables direct entry of bioactive molecules into the systemic circulation with better and easy accessibility, bypassing the hepatic metabolism and improving patient compliance. Permeation through the skin has always been a barrier. To overcome this challenge, an efficient route by the vesicular system has been adopted so as to have better skin permeation of the bioactive molecules. A novel vesicular and non-invasive drug delivery system called Nanoethosomes was developed. Nanoethosomes are lipid-based vesicular carriers that are used for deeper permeation of the bioactive agents into the skin. The main components of Nanoethosomes are Phospholipids, water, and ethanol. High ethanol concentration in Nanoethosomes distinguishes them from other nano-formulation and results in deeper permeation and smaller vesicular size. This review article gives detailed information on the formulation techniques, and characterization parameters of nanoethosomes along with the research work done by various researchers in the same field. The compiled manuscript gives detailed elaboration about the various drugs used to treat different diseases which when incorporated in nanoethosomes resulted in better permeability and enhanced bioavailability.

Naproxen-phospholipid complex, a new vesicular drug delivery system: design, development, and evaluation

Naproxen-phospholipid complex, a new vesicular drug delivery system: design, development, and evaluation

Preparation, In-vitro, and Ex-vivo Evaluation of Ondansetron Loaded Invasomes for Transdermal Delivery

Invasomes are newly developed types of nanovesicles. A vesicular drug delivery system is considered one of the approaches for transdermal delivery to enhance permeation and improve drug bioavailability. Ondansetron is a serotonin receptor antagonist used for treating vomiting associated with different clinical cases. The study aimed to prepare invasomal dispersions for improving permeation of ondansetron across the skin with a controlled release pattern. Twenty-seven formulas of ondansetron-loaded invasomes were prepared by a modified mechanical dispersion method. These formulas were optimized by studying the effect of variables on entrapment efficiency. Vesicle size, polydispersity, zeta potential, in-vitro release and ex-vivo permeation studies were done for the optimized formulas. The selected formula was )F25( had )88.24%±0.04 (entrapment, (317.7 nm) vesicle size, (0.29) polydispersity, and (-31.5mV) zeta potential. In-vitro release study showed That (F25) had 75% release after (12) hrs., and dissolution followed the Korsmeyer-Peppas model with anomalous diffusion. Ex-vivo permeation study showed steady-state flux was 340.2 µg/cm2.hr with no lag time using rat skin tissue. A transmission electron microscope was done to visualize the selected formula. Invasomes are considered promising drug delivery systems for transdermal delivery of ondansetron, ensuring efficient permeation with a sustained release pattern.

Formulation and in-vitro Evaluation of Baclofen loaded Transferosomal Gel

Baclofen is a class of medications called skeletal muscle relaxant. It is a class III drug having low solubility and high permeability used in treating multiple sclerosis symptoms such as spasticity, stiffness, and pain. The current study involves the development and in-vitro evaluation of a Baclofen-loaded transfersomal gel to reduce dosage frequency. Drug and excipient interactions were not detected in the FTIR spectra. Hand shaking modified thin film hydration method was used to developed transfersome formulations, which then consolidated at 0.5% carbopol gel. Optimized BF7 formulation provides higher Entapment efficiency and maximum drug delivery. The prepared formulation had been examined for FTIR, Organoleptic evaluation, Viscosity, Spread-ability, Entrapment Efficacy, Drug content, SEM analysis, Particle size, Zeta potential, Stability testing, and other parameters. The optimised formulation BF7 confirmed Entapment Efficiency ranging from 80.04 to 87.42%, Drug content ranging from 90.26 -95.37%, Vesicle Size of 167.8nm & In-vitro diffusion of 97.48%. The drug release data from the chosen gel demonstrated a good fit with the Higuchis and Zero order release kinetics.
 Keywords: Transferosomes, vesicular drug delivery system, Thin film hydration method

Formulation and Evaluation of Gel Containing Nigella sativa Seed Extract Loaded Transferosomes for Effective Treatment of Psoriasis

Background: Psoriasis vulgaris is an autoimmune associated skin disease causing plaques or scales formation where the skin cells form quicker than in their typical life cycle. The phenolic phytoconstituents reported in Nigella sativa are effective for the treatment of skin disorders. Transfersomes is an emerging nanoencapsulation drug delivery approach which can squeeze themselves due to its elastic nature as an intact vesicle across narrow pores. It improves the potency of topical formulations with higher permeation efficiencies compared to other vesicular drug delivery systems. Objective: This research work focused to prepare Nigella sativa or black seed extract loaded transfersomes as nanoformulation and further incorporating them in the gel system to give improved therapeutic efficacy due to their self-regulating and self-optimizing capabilities. Methods: The phenolic content of Nigella sativa or black seed was extracted in ethanol and the solvent was removed using a vacuum with suitable storage conditions at 22ºC. Transfersomes of ethanol extract were prepared by thin layer hydration method and further incorporated into gel formulations. The ant-psoriasis activity of prepared gel formulation was performed with histopathology study in the Imiquimod induced albino rat model. Results: A nanoformulation prepared with 0.85 mg lecithin and 0.10 mg tween 80 has the highest entrapment efficiency. The entrapment efficiency, vesicle size, polydispersity index and zeta potential of optimized transferosomes batch were found to be 69.3 ± 2.6%, 178 ± 11 nm, 1.1 ± 0.2, -29.4 mV, respectively. Anti-psoriatic activity of N. sativa seed extract loaded transfersomes showed a more significant reduction in thickness of the epidermis and less elongation of rete ridges with capillary loop dilation as compared to conventional gel formulation. Conclusion: We concluded that the Nigella sativa seed ethanolic extract loaded transfersomes gel formulation showed significant ant-psoriasis activity in an albino rat model.

Cubosomes as versatile lipid nanocarriers for neurological disorder therapeutics: a comprehensive review.

Cubosomes are novel vesicular drug delivery systems with lipidic liquid crystal nanoparticles formed of predetermined proportions of amphiphilic lipids. They have a honeycomb-like structure and are thermodynamically stable. These bicontinuous lipid layers are separated into two water-based channels internally that can be used by various bioactive substances, including drugs, proteins, and peptides. This complex structure is responsible for its high drug-loading capacity. Cubosomes are thought to be promising vehicles for various routes of administration because of their extraordinary characteristics, including bioadhesion, the capacity to encapsulate hydrophilic, and hydrophobic, as well as amphiphilic substances, high resistance to environmental stress, and their ability to achieve controlled release through modification. One of the essential elements for improving patient compliance is the ability of these well-defined nano-drug delivery systems to boost the effectiveness of targeting while lowering the side effects/toxicities of payloads. The large internal surface area, a sufficiently uncomplicated fabrication procedure, and biodegradability make it an attractive nano lipid carrier for drug delivery. This review outlines the recent advancement of cubosomes for managing various neurological disorders, highlighting their potential in this field.

The Utilization of Plant-Material-Loaded Vesicular Drug Delivery Systems in the Management of Pulmonary Diseases.

Medicinal plants have been utilized to treat a variety of conditions on account of the bioactive properties that they contain. Most bioactive constituents from plants are of limited effectiveness, due to poor solubility, limited permeability, first-pass metabolism, efflux transporters, chemical instability, and food-drug interactions However, when combined with vesicular drug delivery systems (VDDS), herbal medicines can be delivered at a predetermined rate and can exhibit site-specific action. Vesicular drug delivery systems are novel pharmaceutical formulations that make use of vesicles as a means of encapsulating and transporting drugs to various locations within the body; they are a cutting-edge method of medication delivery that combats the drawbacks of conventional drug delivery methods. Drug delivery systems offer promising strategies to overcome the bioavailability limitations of bioactive phytochemicals. By improving their solubility, protecting them from degradation, enabling targeted delivery, and facilitating controlled release, drug delivery systems can enhance the therapeutic efficacy of phytochemicals and unlock their full potential in various health conditions. This review explores and collates the application of plant-based VDDS with the potential to exhibit protective effects against lung function loss in the interest of innovative and effective treatment and management of respiratory illnesses.

Development of the cholestosome, a novel delivery system made exclusively from cholesteryl esters

AbstractA novel vesicular drug delivery system has been created using only cholesteryl esters. The uncharged nature of the esters requires a formulation process that uses energy, in the form of sonication, to facilitate the cholesteryl esters formation into vesicles. The nature of the material choices renders the vesicles resistant to pH degradation between a pH of 2 and 10. Storage condition at 4°C for 9 months shows a stability of encapsulated materials as well as vesicles. The formulation process is a modified reverse phase method in which the esters are dissolved in an organic solvent, which is then removed and the aqueous component is then added with sonication in a temperature‐controlled water bath. A wide variety of materials can be encapsulated in these vesicles, which are called cholestosomes. Delivery of the cholestosome‐encapsulated materials is a function of the ester component structure and not the encapsulated molecule. Once encapsulated, the vesicles deliver the materials into cells. The potential for oral availability was explored using chylomicrons. Successful delivery of the cholestosome encapsulated into chylomicrons has enhanced the effectiveness of delivery to cells. Analytical methods have been developed to analyze the materials chosen from the cholesteryl esters as well as the encapsulated materials.Practical Applications: The creation of the cholestosome vesicle opens up completely new areas for encapsulating and delivering materials. The cholesteryl ester structure that makes up the vesicles is impervious to pH and bile salts, making cholestosomes ideal for oral delivery of drugs, such as oral insulin. Intracellular delivery of cholestosome vesicles enables multiple applications, from killing latent infections to preventing viral replication (irrespective of the virus) and delivering nucleic acid therapeutics to cure genetic disease. These vesicles pass the blood–brain barrier and could be used for treatments of Alzheimer's and related neurodegenerative disease. Cholestosomes can also be used in cosmetic formulations as the vesicles pass the dermis. They even could be used in food applications as the materials are considered generally regarded as safe.

A comprehensive and updated review on the applications of vesicular drug delivery systems in treatment of brain disorders: A shelter against storms

A comprehensive and updated review on the applications of vesicular drug delivery systems in treatment of brain disorders: A shelter against storms

Vesicular drug delivery systems for oral absorption enhancement

Oral administration is the most acceptable route of drug delivery at this stage due to its convenience, safety, and non-invasiveness. However, drugs given orally are exposed to a complex gastrointestinal environment, causing a tremendous challenge for their successful absorption into the circulation. Over the past decades, researchers have developed various novel pharmaceutical technologies to improve oral absorption, among which the vesicular drug delivery system (like liposomes, niosomes and transfersomes) has received extensive attention. Encouragingly, there have been several investigations confirming the improved effect of vesicular drug delivery systems on oral drug absorption. Nevertheless, the clinical translation of oral vesicular drug delivery systems has been less impressive than implied by the positive results, and few vesicular formulations for oral use have been marketed yet. Against this background, this article provides an overview of the current applications and challenges associated with the vesicular delivery systems available for oral drug delivery, specifically liposomes, niosomes, transfersomes, chitosomes and bilosomes. The composition, formation mechanism, drug delivery advantages and application cases of these carriers in oral drug delivery are summarized. The possible mechanisms by which vesicular carriers enhance oral drug absorption are analyzed in terms of the in vivo process of oral drugs. Further, the challenges that oral vesicular carriers now face, such as safety, undefined in vivo fate, and scale-up production, are summarized, while possible strategies to deal with them are indicated. By reviewing the aforementioned, it can facilitate a more comprehensive knowledge of vesicular systems that can be used for oral drug delivery, providing a theoretical basis and reference for the design of oral formulations.

A critical analysis of the vesicular drug delivery system: recent advancements and prospects for the future

Vesicular system drug design has revitalised the efficacy of previous medications by effectively regulating and sustaining their therapeutic action. The objective of this study is to evaluate the feasibility of utilizing pharmaceutical interventions to target novel vesicular drug delivery systems. The objective of innovative medication administration is to minimize adverse effects while ensuring drug efficacy at a predetermined or reasonably consistent level within the body. A novel drug delivery approach is characterized by the controlled release of medication at a predetermined rate, which is determined based on factors such as therapeutic requirements, pharmacological properties, drug characteristics, physiological condition of the organism, and other relevant considerations. At present, there is a lack of medication delivery technologies that effectively achieve the aforementioned objectives while minimizing adverse effects. The utilization of vesicular systems in drug delivery has brought about changes in the understanding and application of diagnosis and therapy across different domains within the biomedical field. The vesicular drug delivery system (VDDS) serves as a means to address the disparity between the theoretical ideal and the presently accessible innovative drug delivery systems, accomplishing this by enclosing active moieties within vesicular structures. Various vesicular drug delivery systems, such as liposomes, niosomes, transferases, pharmacosomes, colloidosomes, herbosomes, sphinosomes, among others, have been developed. This review primarily focuses on the examination of various pharmacological targets, both lipiodal and nonlipoidal, within vesicular systems. Liposomes and niosomes represent innovative drug delivery systems.

Formulation And Evaluation of Miconazole Pharmacosome by Using Solvent Evaporation Method to Enhance Solubility of Miconazole

This study aims to improve the solubility, bioavailability, and safety profile of miconazole through the development of a pharmacokinetic, a type of vesicular drug delivery system known for its advantages over with conventional methods. Using a solvent evaporation technique, miconazole is encapsulated in a soy lecithin-based pharmacokinetics. The pharmacokinetics obtained showed significant improvements in drug solubility, concentration uniformity and stability. One specific formulation, rated F1, with an exact ratio of miconazole to soy lecithin showed an impressive drug release rate of 94.25% within 60 minutes, in stark contrast to the release rate of only 28.90% achieved by free miconazole. This improved release profile shows the potential to improve treatment efficacy. In addition, both the standard F1 and miconazole formulations exhibited significant antifungal activity against Candida albicans, as evidenced by the minimum inhibitory concentrations (MICs) of 144.23 ?g/ml and 143.31 ?g/ml respectively. The innovative approach of complexing miconazole with soy lecithin through the formation of pharmacokinetics not only enhances drug solubility and bioavailability, but also contributes to minimizing potential toxic effects. These results highlight a promising pharmaceutical role as a means of improving the pharmacological properties of miconazole and other potential drugs with similar solubility challenges. This study has important implications for the development of more effective and safer therapeutic interventions in the field of antifungal therapy.

Sphingosomes: A Novel Vesicular Drug Delivery System

Sphingosomes are bilayer vesicles, primarily made of natural or synthetic sphingolipids, that completely surround an aqueous volume. Sphingosomes address the main issues with vesicle systems (liposomes, niosomes), including their lack of stability, short in vivo circulation times, and poor tumour loading efficacy in cancer therapy. Sphingosomes are a promising vesicular drug delivery system that can transport therapeutic chemicals for a variety of potential applications, according to the review's findings. The development of novel medication delivery systems has received a lot of attention in recent decades (NDDS). To begin, it should administer the medication at a pace determined by the body's requirements throughout the course of therapy. Second, it must direct the active entity to the action location. None of these can be met by conventional-dose forms, including extended-release dosage forms. No existing drug delivery system now acts optimally, although genuine efforts have been made to accomplish them via different new drug delivery methods.1-5