Topical Drug Delivery Systems Research Articles

Basic components and formulation aspect of transdermal patches: A topical novel drug delivery system

Basic components and formulation aspect of transdermal patches: A topical novel drug delivery system

Preparation of an injectable zinc-containing hydrogel with double dynamic bond and its potential application in the treatment of periodontitis.

Periodontal tissue regeneration continues to face significant clinical challenges. Periodontitis leads to alveolar bone resorption and even tooth loss due to persistent microbial infection and persistent inflammatory response. As a promising topical drug delivery system, the application of hydrogels in the controlled release of periodontal bioactive drugs has aroused great interest. Therefore, the design and preparation of an injectable hydrogel with self-repairing properties for periodontitis treatment is still in great demand. In this study, polysaccharide-based self-healing hydrogels with antimicrobial osteogenic properties were developed. Zinc ions are introduced into a dynamic cross-linking network formed by dynamic Schiff bases between carboxymethyl chitosan and oxidized hyaluronic acid via coordination bonds. The OC-Zn hydrogels exhibited good tissue adhesion, good fatigue resistance, excellent self-healing ability, low cytotoxicity, good broad-spectrum antimicrobial activity, and osteogenic activity. Therefore, the designed hydrogels allow the development of drug delivery systems as a potential treatment for periodontitis.

Emulgel Towards Novel Formulation Development: A Comprehensive Review

Emulgels are an innovative topical drug delivery system that combines the properties of emulsions and gels to enhance the delivery and efficacy of pharmaceuticals. These systems leverage the advantages of both components: the solubilizing capabilities of emulsions and the stable, bioadhesive properties of gels. This review aims to summarize the development, formulation strategies, evaluation techniques, and therapeutic applications of emulgels. A comprehensive literature search was conducted across various scientific databases including PubMed, Scopus, and Web of Science. Studies focusing on the formulation, characterization, and clinical efficacy of emulgels were included. The review evaluates the methodologies used in the preparation of emulgels, including the choice of gelling agents, emulsifiers, and active pharmaceutical ingredients (APIs). Analytical techniques for assessing the physicochemical properties and stability of emulgels were also examined. The review identified key formulation parameters that influence the performance of emulgels, such as the type and concentration of gelling agents (e.g., carbomers, xanthan gum), emulsifiers (e.g., Tween, Span), and oils. Optimization of these components significantly affects the viscosity, spreadability, and drug release profile of emulgels. Studies demonstrated that emulgels exhibit improved drug penetration and sustained release compared to conventional topical formulations. Therapeutic applications of emulgels encompass a wide range of conditions including dermatological disorders, pain management, and microbial infections. The review also highlights novel advancements such as the incorporation of nanoparticles and the development of stimuli-responsive emulgels. Emulgels represent a promising platform for topical drug delivery, offering enhanced stability, bioavailability, and patient compliance. The versatility in their formulation allows for the incorporation of diverse APIs, making them suitable for various therapeutic areas. Future research should focus on the clinical translation of emulgels, exploring their potential in personalized medicine, and addressing regulatory challenges. Emulgels have the potential to revolutionize topical therapy and provide new avenues for effective and targeted 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.

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.

Overview on Emulgel and their marketed Formulations

Background: Emulgel is a topical preparation prepared by the mixture of an emulsion and a gel. Emulgel is considered as one of the most important topical delivery systems because it consists of two release control systems, i.e., a gel and an emulsion. The primary intention of this new topical delivery system is to deliver hydrophobic drugs into systemic circulation through the skin. By applying a suitable statistical design, different grades of emulgel can be prepared. There are various favorable properties. Therefore, emulgel is considered as the most conventional system available in the market over other topical drug delivery systems. Objectives: In the present work an attempt was made to prepare emulgel of garlic oil and ajwain oil for enhancing its topical delivery. Material and Method: Emulgel formulation was characterized by various parameters like pH, viscosity, spredability, Extrudability, microbiological Assay.

Enhanced topical paromomycin delivery for cutaneous leishmaniasis treatment: Passive and iontophoretic approaches

Conventional treatments for cutaneous leishmaniasis, a neglected vector-borne infectious disease, can frequently lead to serious adverse effects. Paromomycin (PAR), an aminoglycoside antibiotic, has been suggested for the topical treatment of disease-related lesions, but even when formulated in high drug-loading dosage forms, presents controversial efficacy. The presence of five ionizable amino groups hinder its passive cutaneous penetration but make PAR an excellent candidate for iontophoretic delivery. The objective of this study was to verify the feasibility of using iontophoresis for cutaneous PAR delivery and to propose a topical passive drug delivery system that could be applied between iontophoretic treatments. For this, in vitro iontophoretic experiments evaluated different application durations (10, 30, and 360 min), current densities (0.1, 0.25, and 0.5 mA/cm2), PAR concentrations (0.5 and 1.0 %), and skin models (intact and impaired porcine skin). In addition, 1 % PAR hydrogel had its penetration profile compared to 15 % PAR ointment in passive transport. Results showed iontophoresis could deliver suitable PAR amounts to dermal layers, even in short times and with impaired skin. Biodistribution assays showed both iontophoretic transport and the proposed hydrogel delivered higher PAR amounts to deeper skin layers than conventional ointment, even though applying 15 times less drug. To our knowledge, this is the first report of PAR drug delivery enhancement by iontophoresis. In summary, the association of iontophoresis with a topical application of PAR gel seems appropriate for improving cutaneous leishmaniasis treatment.

Targeting Potential of Zinc Oxide Nanoparticles and Finasteride-loaded Nano Lipidic Carriers-infused Topical Gel - In vitro and In vivo Skin Permeation Studies

Background: There is an unmet clinical need to develop topical carriers for finasteride to reduce its systemic side effects in the treatment of androgenic alopecia (AGA). Zinc oxide (ZnO) nanoparticles have also emerged as an influential agent in hair biology. Aim: The main focus of the work was to develop a novel formulation to explore the potential of ZnO nanoparticles in combination with NLCs of finasteride (FIN) for topical delivery. Method: ZnO nanoparticles were synthesized by precipitation method and were subsequently incorporated within the Carbopol gel. The ZnO nanoparticles and the gel were evaluated for their physicochemical characteristics. In vitro release study was performed for the determination of release of the drugs from the gel and ex vivo study was conducted for the determination of penetration of the NLCs and ZnO nanoparticles into the skin. Result: The particle size of the nanoparticles was found to be 200 nm. The pH, viscosity and spreadability of the gel was observed to be 6.13±2.11, 35,845.3±6.97 cps at 5 rpm and 17.14±2.32 respectively. Ex vivo drug permeation and skin distribution studies of the NLC gel formulations carried on rat dorsal skin indicated 25.763±0.2 μg/cm² and 19.375±1.2 μg/cm² of FIN and ZnO in 12 hr respectively. Conclusion: The results indicated the potential of developed systems for topical drug delivery for treatment of androgenic alopecia.

Preparation and Characterization of an Antiviral Gel

The study was to develop an antiviral gel for topical application. The topical application of drug has many advantages over the intravenous and oral administration. It prevents metabolism of drug from liver and avoid the risk of gastrointestinal disorder and inconvenience of intravenous therapy pain. When the drug is applied topically it can penetrate deeper into the skin hence show better absorption and bioavailability. The wide varieties of pharmaceutical dosage form are available for topical drug delivery system. The most used one is gel, ointment and cream. Herpes Simplex Virus (HSV) is widely spread that cause infections. There are two types of this virus, one is HSV-1 usually causes sore around the lip or inside the mouth that are sometime called fever blisters or cold sore and the second is HSV-2, it causes sore on the genitals. Acyclovir is a selective and effective antiviral agent. Acyclovir remains the gold standard in the treatment of Herpes Simplex Virus infections, mainly due to emerging new drug delivery systems which are improving the bioavailability and fewer side effects. The gel was prepared in different batches or formulation by using different types of polymers in varying concentration viz. Carbopol-934, Carbopol-940, HPMC, and Na The gel formulations were evaluated for physical and chemical characterization like visual appearance, drug content, pH, viscosity, extrudability, spread ability etc. and the results was compared.

Effect of Pretreatment Time with Enhancers on Caffeine Skin Permeability in Rats

Background: Caffeine is an edible chemical compound obtained from various plants, such as tea and coffee. Caffeine is an alkaloid that is highly hydrophilic and has limited skin permeability. The lipophilic nature of the stratum corneum is a major barrier to the passage of this substance through the skin. Topical drug delivery systems can effectively transfer caffeine to the skin. Objectives: This study investigated the effect of pretreatment time with chemical enhancers on caffeine's skin permeation. Methods: The skin was subjected to additives such as sodium lauryl sulfate, sodium lauryl ethyl sulfate, tynoline, nanoxinol, and lecithin for 5, 15, and 30 minutes. Then, the parameters of caffeine permeability and structural changes in the skin due to additive adsorption were studied using Fourier Transform Infrared (FT-IR) spectrometry. Results: The enhancers increased the permeation of caffeine through the skin. There are different mechanisms for penetration enhancers, including lipid liquefaction, disruption of lipid bilayers, and irreversible denaturation of intracellular keratin. Conclusions: Sodium lauryl sulfate can affect the skin permeability of caffeine.

WITHDRAWN: Formulation and evaluation of Ferulic acid and Oleic acid containing liposomal gel for skin nourishment

AimThis study aimed to develop a topical drug delivery system using a liposomal gel loaded with Ferulic acid and Oleic acid, with a dual focus on the treatment of aging skin and skin nourishment. ObjectivesTo formulate liposomes containing Ferulic acid and Oleic acid via the thin-film hydration technique. To incorporate the optimized liposomes into a Carbopol® 934 gel matrix. To comprehensively characterize the physicochemical properties of the liposomes and liposomal gel. To evaluate the potential of the developed liposomal gel as an efficacious topical solution for addressing skin aging and promoting skin nourishment. MethodsLiposomes were meticulously prepared using the thin-film hydration technique and were subsequently integrated into a Carbopol® 934 gel matrix. A range of crucial assessments were conducted, encompassing entrapment efficiency, drug loading, particle size, polydispersity index (PDI), and zeta potential. The physicochemical attributes of both the liposomes and liposomal gel were systematically examined. The study also sought to evaluate the potential of the liposomal gel for its dual role in combating skin aging and enhancing skin nourishment. ResultsThe optimized liposomes exhibited remarkable characteristics, including an entrapment efficiency of 95.1%, drug loading of 67.5%, a particle size of 1028 ​nm, a polydispersity index (PDI) of 0.488, and a zeta potential of -49 mV. These parameters underscored the successful formulation of Ferulic acid and Oleic acid-loaded liposomes, which were seamlessly incorporated into the Carbopol® 934 gel matrix. ConclusionIn conclusion, the Ferulic acid and Oleic acid-loaded liposomal gel developed in this study holds significant promise as a topical drug delivery system for both the treatment of aging skin and skin nourishment. The high entrapment efficiency, substantial drug loading, and desirable particle size and zeta potential collectively demonstrate the efficacy of this liposomal gel as a versatile delivery platform. It has the potential to effectively address clinical manifestations of aging skin, including wrinkles, loss of elasticity, and textural irregularities, while simultaneously providing essential nourishment to the skin. Further in vivo investigations are warranted to ascertain the therapeutic effectiveness and safety of this liposomal gel in the context of skin aging treatment and nourishment.

Mucoadhesive and thermosensitive Bletilla striata polysaccharide/chitosan hydrogel loaded nanoparticles for rectal drug delivery in ulcerative colitis

Ulcerative colitis (UC) is a chronic disease with diffuse mucosal inflammation limited to the colon. A topical drug delivery system that could be facilely performed and efficiently retained at colon are attractive for clinical ulcerative colitis treatment. Herein, a novel platform for rectal administration of thermosensitive hydrogel co-loaded with nanoparticles to treat ulcerative colitis was developed. Thiolated-hyaluronic acid was synthesized, and prepared nanoparticles with zein and Puerarin. And the Bletilla striata polysaccharide with colonic mucosa repair effect was oxidized, and mixed with chitosan and β-sodium glycerophosphate to prepare thermosensitive hydrogel. Thermosensitive hydrogels were combined with nanoparticles to investigate their mucosal adhesion, retention, and permeability, as well as their therapeutic effects on ulcerative colitis. Thiolated-hyaluronic acid nanoparticles had good stability, and could be quickly converted into hydrogel at body temperature when combined with thermosensitive hydrogel. The nanoparticles-loaded thermosensitive hydrogel also was excellent at mucosal penetration, enhancing the retention time of drugs in colon, and effectively controlling drug release. In vivo ulcerative colitis treatment revealed that the nanoparticles-loaded hydrogel significantly repaired the colonic mucosa and inhibit colonic inflammation. Therefore, the thermosensitive hydrogel co-loaded nanoparticles will have a promising application in effective treatment of ulcerative colitis by topical administration.