Topical Drug Delivery Systems Research Articles

Revolutionizing Knee Osteoarthritis Treatment: Innovative Self-Nano-Emulsifying Polyethylene Glycol Organogel of Curcumin for Effective Topical Delivery.

In the current study, self-nano-emulsifying (SNE) physically cross-linked polyethylene glycol (PEG) organogel (SNE-POG) as an innovative hybrid system was fabricated for topical delivery of water-insoluble and unstable bioactive compound curcumin (CUR). Response surface methodology (RSM) based on Optimal Design was utilized to evaluate the formulation factors. Solid fiber mechanism with homogenization was used to prepare formulations. Pharmaceutical evaluation including rheological and texture analysis, their mathematical correlations besides physical and chemical stability experiments, DSC study, in vitro release, skin permeation behavior, and clinical evaluation were carried out to characterize and optimize the SNE-OGs. PEG 4000 as the main organogelator, Poloxamer 188 (Plx188) and Ethyl Cellulose (EC) as co-gelator/nanoemulsifier agents, and PEG 400 and glycerin as solvent/co-emulsifier agents could generate SNE-POGs in PS range of 356 to 1410 nm that indicated organic base percentage and PEG 4000 were the most detrimental variables. The optimized OG maintained CUR stable in room and accelerated temperatures and could release CUR sustainably up to 72 h achieving high flux of CUR through guinea pig skin. A double-blind clinical trial confirmed that pain scores, stiffness, and difficulty with physical function were remarkably diminished at the end of 8 weeks compared to the placebo (71.68% vs. 7.03%, 62.40% vs. 21.44%, and 45.54% vs. 8.66%, respectively) indicating very high efficiency of system for treating knee osteoarthritis. SNE-POGs show great potential as a new topical drug delivery system for water-insoluble and unstable drugs like CUR that could offer a safe and effective alternative to conventional topical drug delivery system.

A review on topical ophthalmic drug delivery system: Reference to viscosity enhancer.

The eye is the most accessible site for topical drug delivery. Drug's ocular bioavailability is quite low when administered topically as eye drops. Viscosity enhancers are used to increase ocular bioavailability by extending the precorneal residence time of the drug at the ocular site. Cellulose, polyalcohol and polyacrylic acid are examples of hydrophilic viscosity enhancers. The addition of viscosity modifiers increases the amount of time the drug is in contact with the ocular surface. Several polysaccharides have been studied as excipients and viscosity boosters for ocular formulations, including cellulose derivatives such as chitosan (CS), xyloglucan and arabinogalactan (methylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose (HPMC), and sodium carboxymethylcellulose). Viscosity-increasing substances reduce the surface tension, extend the corneal contact time, slow the drainage, and improve the bioavailability. Chitosan is a viscosity enhancer that was originally thought to open tight junction barrier cells in the epithelium. Chitosan thickens the medication solution and allows it to penetrate deeper. Alginate is an anionic polymer with carboxyl end groups that has the highest mucoadhesive strength and is used to improve penetration. Carboxymethylcellulose (CMC), a polysaccharide with a high molecular weight, is one of the most common viscous polymers used in artificial tears to achieve their longer ocular surface residence period. Hyaluronic acid (HA) is biocompatible and biodegradable in nature, and it is available in ocular sustained-release dose forms. A polymer known as xanthan gum is used to increase viscosity. At 0.2% concentration, carbomer forms a highly viscous gel.

Design of liposomal nanocarriers with a potential for combined dexamethasone and bevacizumab delivery to the eye

Clinicians face numerous challenges when delivering medications to the eyes topically because of physiological barriers, that can inhibit the complete dose from getting to the intended location. Due to their small size, the ability to deliver drugs of different polarities simultaneously, and their biocompatibility, liposomes hold great promise for ocular drug delivery. This study aimed to develop and characterise a dual loaded liposome formulation encapsulating Bevacizumab (BEV) and Dexamethasone (DEX) that possessed the physicochemical attributes suitable for topical ocular delivery. Liposomes were prepared by using thin film hydration followed by extrusion, and the formulations were optimised using a design of experiments approach. Physicochemical characterisation along with cytocompatibility and bioactivity of the formulations were assessed. Liposomes were successfully prepared with a particle size of 139 ± 2 nm, PDI 0.03 ± 0.01 and zeta potential −2 ± 0.7 mV for the optimised formulation. BEV and DEX were successfully encapsulated into the liposomes with an encapsulation efficiency of 97 ± 0.5 % and 26 ± 0.5 %, respectively. A sustained release of BEV was observed from the liposomes and the bioactivity of the formulation was confirmed using a wound healing assay. In summary, a potential topical eye drop drug delivery system, which can co-load DEX and BEV was developed and characterised for its potential to be used in ocular drug delivery.

Technical Considerations, Applications, and Benefits of Organogels in Topical Drug Delivery Systems.

Organogels represent semi-solid systems where an organic liquid phase is entrapped within a three-dimensional network formed by self-assembled, crosslinked, or entangled gelator fibers. These versatile materials find applications in a wide range of fields, including chemistry, pharmaceuticals, cosmetics, biotechnology, and food technology. Notably, in pharmacology, they serve as valuable platforms for drug and vaccine delivery, facilitating the transport of active ingredients through various routes such as transdermal, oral, and parenteral. However, their previous utility as drug delivery systems was hindered by the toxicity associated with the organic solvents used. The pharmacokinetics of medications delivered via organogels are primarily influenced by the distinctive properties of these materials, specifically their "high permeability and poor aqueous solubility," which can impact the bioavailability of the drugs. Organogels can be employed topically or for the controlled release of medications through cutaneous administration and percutaneous absorption, expanding their scope of application beyond conventional drug delivery methods. Organogels hold significant promise as drug delivery vehicles due to their biocompatibility, non-irritating properties, and thermoremanent characteristics. They enable the formulation of diverse drug delivery systems by incorporating both hydrophilic and hydrophobic bioactive compounds within the gel matrix. This comprehensive review offers an overview of organogels, encompassing their nature, synthesis, characterization, and properties. Special attention is directed towards cutting-edge technologies employed in designing organogels as potential controlled delivery systems, with a focus on their emerging therapeutic applications.

Potential inhibition of CXCL12/SDF-1 by small molecule Hesperetin in management of tobacco associated oral cancer

Goal of the perspective: Stromal cell-derived factor-1 alpha CXCL12/SDF-1 has a substantial impact on the tumorigenicity in tobacco related oral cancer. Inhibition could help derive preventive and therapeutic approaches. DiscussionBinding energy score between CXCL12/SDF-1 and small molecule Hesperetin is indicative of a strong and stable interaction, significative of a high affinity for the chemokine. The specific molecular interactions, including hydrogen bonding and van der Waals interactions further contribute to the stable complex formation. ConclusionTargeting molecular components of the NF-κB signaling pathway through inhibition of CXCL12/SDF-1 could serve as a vital therapeutic adjunct in management of tobacco associated oral cancer. Also topical drug delivery systems with Hesperetin can be planned in oral potentially malignant disorders.

A Review on Effective Treatment of Chronic Skin Allergy using Chlorpheniramine

Allergies, is a bunch of medical circumstances caused by the hypersensitivity of the immune system to typically harmless substances in the environment. Allergy can be a type of hay fever, food allergies, atopic dermatitis, allergic asthma, and anaphylaxis. Symptoms of allergy include red eyes, an itchy rash, sneezing, coughing, a runny nose, shortness of breath, or swelling. Antihistaminics are very useful candidates to treat allergy. The dose of antihistaminics can be reduced by local administration of anti-histaminics at the site of allergy. Skin allergy is basically related to dermal site of the skin it replicates to other organ near or in contact with skin. Administration of chlorpheniramine directly to the shin as topical drug delivery system will help to reduce the skin allergies.

Emulgel: A Cutting Edge Approach for Topical Drug Delivery System.

Emulgel is considered an advanced leading form of topical drug delivery system. It possesses the quality of a dual control drug mechanism for drug release as it holds the properties of both gel as well as emulsion. Emulgel is capable of overcoming the problems of the conventional route of topical drug delivery, like low spreadability and stickiness with the delivery of hydrophobic drugs, enhanced bioavailability at the local site of action, no greasy texture, and ensuring patient compliance. An emulsion is used either w/o or o/w, and the drug can be incorporated into the suitable phase of the emulsion. After that, the emulsion is incorporated into the gel phase. Several factors like oil phase, gelling agent, and emulsifier can affect the efficacy and stability. This advancement is beneficial not only for dermatology but also for cosmetology as well. Currently, emulgel-based formulations are used for the delivery of anti-inflammatory, analgesic, anti-acne, and antifungal drugs with a wide array of exploration.

Formulation and In Vitro Evaluation of Niosomal Gel for The Topical Administration of Losartan Potassium

This study aims to develop and test a topical drug delivery system for antihypertensive activity using Losartan potassium-loaded niosomes. The niosomes were created using the traditional ether injection approach, with four formulations made using cholesterol as the lipid and varying quantities of surfactants such as span 80 and span 60. The different formulations underwent testing for FTIR, particle size, zeta potential, drug content, entrapment efficiency, and in vitro release. FTIR analysis revealed that the medication was incompatible with excipients. The study concludes by highlighting current obstacles and future possibilities for the development of niosomes as effective vehicles. Overall, this analysis provides insight into the potential of niosomes in medication delivery and encourages further research in this field.
 Keywords: Losartan potassium, Antihypertensive, Niosomes, Tween 80 and Span 20

A Review on Novel Film Forming Systems for Topical and Transdermal Drug Delivery

A Review on Novel Film Forming Systems for Topical and Transdermal Drug Delivery

Proniosomal gel mediated transdermal delivery of Donepezil HCl: Development and in vitro characterization

The aim of this research was to study the potential of proniosomal gel for transdermal delivery. Donepezil HCl loaded proniosomal gels were prepared by the coacervation phase separation method using different nonionic surfactants (spans and tweens). The prepared Donepezil HCl proniosomal gels were evaluated for various parameters such as particle size (PS), drug entrapment efficiency percentage (EE %), and in vitro drug release. Donepezil HCl loaded proniosomal gel was prepared successfully by coacervation phase separation method. The prepared proniosomal gel exhibited desired entrapment efficiency and Particle size. It was found that B2 which chosen as a best formula according to entrapment efficiency, Particle size, and in vitro release study. It was found that B2 which contains high concentration of span 60 is the most appropriate surfactant for the preparation of proniosomes. In vitro release studies proved that the prepared proniosomal gel contains Donepezil HCl considered to be a successful topical transdermal drug delivery system and provide a sustained release of encapsulated drug. Furthermore, there was no significant change in EE % and PS of Donepezil HCl proniosomal gel after storage for 6 months.

A Review on Oleogels and its Role in Pharmaceutical Field

Gel-based products called oleogels due to their required rheological, physical, and chemical stabilities in semisolid formulations not only have wide applications in the cosmetic industry, and nutraceutical industries but also they are used largely in various pharmaceutical field for formulating various topical drug delivery system and also as oil-based gels as versatile drug delivery systems for paediatric purpose. Oleogels are semisolid non-crystalline, thermo-reversible viscoelastic systems which consist of a lipophilic liquid phase (mineral or vegetable oils, isopropyl myristate) gelled with a suitable gelling agent referred as organogelators which can improve drug penetration through the stratum corneum because of their lipophilic nature. The polar phase gets trapped inside the three-dimensional networked structure present in the oleogels system, which is formed due to physical interactions among the self-assembled structures of organogelators. As these systems are resistant to the effects of moisture and do not require the addition of stabilizers or preservatives and hence they are preferred in drug delivery systems over conventional gels. The present article focuses on components, formulation aspects, and recent role of oleogels products showing its pharmaceutical applications.

Developments in Emerging Topical Drug Delivery Systems for Ocular Disorders.

According to the current information, using nano gels in the eye has therapeutic benefits. Industry growth in the pharmaceutical and healthcare sectors has been fueled by nanotechnology. Traditional ocular preparations have a short retention duration and restricted drug bioavailability because of the eye's architectural and physiological barriers, a big issue for physicians, patients, and chemists. In contrast, nano gels can encapsulate drugs within threedimensional cross-linked polymeric networks. Because of their distinctive structural designs and preparation methods, they can deliver loaded medications in a controlled and sustained manner, enhancing patient compliance and therapeutic efficacy. Due to their excellent drugloading capacity and biocompatibility, nano-gels outperform other nano-carriers. This study focuses on using nano gels to treat eye diseases and provides a brief overview of their creation and response to stimuli. Our understanding of topical drug administration will be advanced using nano gel developments to treat common ocular diseases such as glaucoma, cataracts, dry eye syndrome, bacterial keratitis, and linked medication-loaded contact lenses and natural active ingredients.

Leptospermum honey – A medicinal wonder for periodontal health

Antibacterial therapy has always been included effectively in the regimen of periodontitis. The inability to access periodontal disease-causing organisms within periodontal pockets has limited the effectiveness of mechanical plaque removal and the use of antibacterial agents. The drug’s systemic administration results in therapeutic concentrations at the site of infection, but only in the short term, necessitating repeated dosing over longer periods. Topical antibiotics have been studied for their ability to overcome the limitations of conventional therapy. It is of interest to use sustained release formulations to deliver antimicrobial agents to the site of infection (periodontal pocket). At much lower doses, these products provide long-term treatment at the site of infection. From time immemorial, honey is not only considered as a natural sweetener but is also used for its healing power. It is used in traditional folk and tribal medicines and 93% of the consumers of honey use it for its medicinal value. Active Leptospermum Honey (ALH) is the most researched medical grade honey for wound and burn treatment. This article documents the efficacy of ALH as a topical drug delivery system in patients with chronic periodontal disease.

Development and Evaluation of Emulgel Formulation of Diclofenac Sodium utilizing Lipidium sativum as a Gelling Agent

Emulgels have gained recognition as an effective method for delivering non-polar drugs. The primary goal of our current research is to investigate the potential of Lepidium sativum seed mucilage as a gelling agent in this context. To enhance drug penetration, we have incorporated clove oil, oleic acid, and methyl salicylate. An emulsion was formulated and subsequently integrated into the gel base. Our research encompassed a series of studies, including rheological assessments, spreading coefficient evaluations, investigations into skin irritancy, and other relevant tests. Furthermore, we conducted drug content analysis, in-vitro release and permeation studies, and stability assessments. In our in-vitro investigations, it was observed that formulation E6 exhibited the highest drug release within a span of 180 minutes. Comparative analyses were conducted, pitting formulations E4, E5, and E6 against a commercially available emulgel preparation. As a result of our findings, it is evident that an emulgel employing L. sativum mucilage can effectively function as a gelling agent in a topical drug delivery system.

Microemulgel-based Hydrogel of Diclofenac Sodium using Lipidium sativum as a Gelling Agent

Aim was to prepare hydrogel containing diclofenac sodium using Lipidium sativum as a gelling agent within a micro emulsion-based system. The oil phase consisted of soybean oil, while surfactants, namely Span 80 and Tween 20, were employed in the formulation. Absolute ethanol was used as a co-surfactant and were characterized by a phase diagram. The in-vitro permeation information is derived from the Franz diffusion. Different microemulsion was designed by screening of various components by performing pseudo-ternary phase diagram and then a solubility study. From this psudo-ternary phase diagram was constructed. In-vitro permeation data was screened from these results the topical delivery of diclofenac sodium microemulsion was clearly confirmed as being by means of w/o microemulsion systems. The optimized formulation of the microemulsion consist of soya bean oil 1.25 mL, span:Tween 20 : 2.5 mL, ethanol 1-mL, water 0.2 mL, L. sativum mucilage and it is compared with the marketed preparation. So, the micro emulsion-based hydrogel of diclofenac using L. sativum mucilage can be used as a gelling agent for a topical drug delivery system.

Evaluation of therapeutic effects of nanofibrous mat containing mycophenolate mofetil on oral lichen planus: In vitro and clinical trial study

Objectives Recently, topical drug delivery system has gained increasing interest in the treatment of oral lesions. Lichen planus is a chronic inflammatory disease affecting mucous membranes and skin. The current study aimed to fabricate a drug delivery system containing mycophenolate mofetil for the treatment of oral lichen planus lesions. Methods Firstly, a nanofibrous mat containing mycophenolate mofetil, zinc oxide nanoparticles, and aloe vera was designed and fabricated. The antimicrobial, cytocompatibility, anti-inflammatory, and antioxidative characteristics of fabricated scaffolds were evaluated. Then, this nanofibrous mat was applied to 12 patients suffering from bilateral erythematous/erosive Oral Lichen planus (OLP) lesions for 2 weeks. The treatment outcomes, including oral symptoms and lesion size, were compared with the routine topical treatment of these lesions; Triamcinolone ointment. Results The characterization of nanofibrous mat approved the successful fabrication of scaffolds. The fabricated nanofibers showed notable antimicrobial activity. The amounts of TNF 𝛼, IL6, and reactive oxygen species (ROS) of stimulated human gingival fibroblasts were decreased after exposure to NFs/Myco/Alv/ZnO scaffolds. The clinical trial results demonstrated the same therapeutic effects compared to the commercial ointment, while the symptoms of patients were significantly improved in the mats group. Significance. Considering the successful results of this study, the application of nanofibrous mat can be a promising product for improving treatment outcomes of OLP.

Development and characterization of topical gel containing deep eutectic mixture of luliconazole for topical drug delivery system

Tinea infections are one of the most occurring dermatophyte infection in the world and more so in tropical countries. It majorly infect children which may lead to them being segregated and shunned away from the community thereby affecting their psychological state. To prepare topical gel containing deep eutectic mixture of luliconazole heating and dispersion method were utilised, and it comprised several steps. The main focus was to improve the solubility as well as the permeability of the drug as it comes into contact with the skin. Choline bitartrate was used as a hydrogen bond donor (HBD), Gallic acid which is a carboxylic acid was used as a hydrogen bond acceptor (HBA), Carbopol 984NF a carbomer was used as a gelling agent. A combination of choline bitartrate and gallic acid in the ratio expressed by formulation code N3 was used for the final preparation. The final properties of the gel; viscosity, spreadability and the drug release profile of the prepared gel were investigated. The drug release of the prepared formulation was compared to the marketed formulation. 4 formulations were prepared using different ratios of the excipients and the optimized formulations were subjected to characterization. Viscosity of the tablet was controlled by amount of gelling agent used in the manufacturing process. Following FTIR studies, it was found that there were no interaction between the drug and the excipients and that the drug release depended on the type of the excipients used in the formulation. Dispersion method was found to be a suitable, easy and efficient technique for designing Topical gel containing deep eutectic mixture (DEM) for topical use.

Enhancement of Curcumin's Anti-Psoriatic Efficacy via Formulation into Tea Tree Oil-Based Emulgel.

Psoriasis is a chronic inflammatory skin disease characterized by the hyperproliferation and aberrant differentiation of epidermal keratinocytes. It is a debilitating condition that can cause significant physical and emotional distress. Natural anti-psoriatic agents have been investigated as alternatives to conventional allopathic medications, as they have notable limitations and drawbacks. Curcumin and tea tree oil are cost-efficient and effective anti-inflammatory medicines with less adverse effects compared to synthetic psoriasis medications. Our research endeavors to harness the therapeutic potential of these natural compounds by developing an herbal anti-psoriatic topical drug delivery system. This novel method uses curcumin and tea tree oil to create a bi-phasic emulgel drug delivery system. Formulations F1 (gel) and F2 (emulgel) have high drug content percentages of 84.2% and 96.7%, respectively. The emulgel showed better spreadability for cutaneous applications, with a viscosity of 92,200 ± 943 cp compared to the gel's 56,200 ± 1725 cp. The emulgel released 94.48% of the drugs, compared to 87.58% for the gel. These formulations conform to the zero-order and Higuchi models, and their stability over a three-month period is crucial. In vivo, the emulgel healed psoriasis symptoms faster than the usual gel. The gathered results confirmed the emulgel's potential as a drug delivery method, emphasizing the complementary benefits of tea tree oil and curcumin as an effective new therapy for psoriasis.

Formulation and Evaluation of Herbal Emulgel: A Review Article

Topical Drug Delivery System Drug: The application of a medication containing formulation for the skin in order to treat the cutaneous condition directly is known as topical drug delivery. Factors Affecting Topical Drug Delivery System: Physiological factors are Skin condition, Lipid content, Blood flow, Skin hydration, Skin temperature and Physiochemical factors are partition coefficient, Molecular weight, Drug concentration, Effect on vehicles. Physiology of Skin: Skin consists of Epidermis Dermis Subcutaneous Tissue. Epidermis is composed basically of: Keratinocytes, Melanocytes, Langerhans cells. Introduction: Emulgels are emulsions oil-in-water or water-in-oil that are combined with an emulsifying agent to form gels. Emulgel is made up of two components: Emulsion: An emulsion is a biphasic system made up of two immiscible liquids, which is one of finely and consistently propagated as globules throughout the other to form an emulsion. Gel: According to the U.S.P., gels are semisolid systems made up of a dispersion whether large organic molecules or small inorganic particles that are encased and penetrated by liquid. Characterization and Evaluation of Herbal Emulgel: Physical Appearance, pH, Viscosity study, Spreadability, Total Ash Value, Loss on drying, In-vitro Diffusion Study. Conclusion: The dosage forms are enhancing topical drug delivery of natural drugs for various topical problem.

A Review on Nanofiber for Topical Drug Delivery of Therapeutic Skin Disorder

Nanofibers for topical drug Delivery of Therapeutic Skin Disorders are the Provide Physiological and Machincal Support to the underlying Cells and oragns any kind of damage and Infection can kind of damage and Infection can destroy this Protective layer. They also some skin disorders like. A Topic, dermaritis, Ichthyosis, Acne, Vitillgo etc. A Nanomaterial with one dimension under 100nm is called a nanofiber. They are the various Properties also include: thermal Properties, Mechanical, Physical are Properties are the include. Some drug loading Method also added like, Blend Elcetrospinning, Coaxial, Immobilizing after electrospinning are the method are loading metho use. And also the Manufacturing of Nanofiber are the added one of the Most Popular method. they also the Critical Parameter of Electrospinning Process like, Surface tension and Viscosity, Applied Voltage, Needle and Collector Distance are the Process include. Nanofiber are the using some various Material of Polymeric (1) Natural Polymers (2) Synthetic Polymers are using. they also some therapeutic application of Nanofiber(1) Nanofibers in wound healing and surgical (2) Nanofiber in treatment of fungal infection (3) Nanofiber in treatment of Acne. (3) Nanofiber in treatment of Skin Cancer. and last one added Electrospun Nanofiber as topical drug delivery system how to the added favourable some Characteristics.