Topical Route Research Articles

Fabrication and Synthesis of Thiococlchicoside Loaded Matrix Type Transdermal Patch.

The goal of this work was to synthesize and fabricate matrix type transdermal patches based on a combination of polymers (Eudragit L100, HPMC and PVP K30), plasticizer and crosslinking agents (propylene glycol and triethyl citrate) and adhesives (Dura Tak 87-6908) to increase Thiocolchicoside (THC) absorption via topical route. This method allows avoidance of first-pass metabolism along with a consistent and extended duration of therapeutic activity. Fabrication and casting of polymeric solutions containing THC was done either in petri plates or through lab coater to get transdermal patches. Finally, the formulated patches were studied for their physicochemical and biological evaluation using scanning electron microscopy, FTIR, DSC, XRD and ex-vivo permeation studies using pig ear skin. FTIR studies confirm that the THC characteristics peaks (carbonyl (Amide I) at 1525.5 cm-1, C=O stretching (tropane ring) at 1664.4 cm-1, Amide II band (N-H stretching) at 3325.9 cm-1, thioether band at 2360.7 cm-1, and OH group stretching band at 3400.2 cm-1) are still present in the polymer mixture even after formulation as a transdermal patch, indicating compatibility among all excipients. While on the other hand, DSC studies confirm endothermic peaks for all the polymers along with THC with the highest enthalpy of 65.979 J/g, which is an indicator of sharp endothermic peak at 198°C, leading to the melting of THC. The percentage drug content and percentage moisture uptake of all the formulation was found in the range of 96 ± 2.04 to 98.56 ± 1.34% and 4.13 ± 1.16 to 8.23 ± 0.90%, respectively. Drug release and release kinetics studies confirm that it is dependent on the composition of individual formulation. All these findings support the possibility of using suitable polymeric composition, as well as proper formulation and manufacturing circumstances, to create a one-of-a-kind technology platform for transdermal drug administration.

High mobility group box 1 cytokine targeted topical delivery of resveratrol embedded nanoemulgel for the management of atopic dermatitis.

Resveratrol is a polyphenolic compound showing anti-inflammatory activity by inhibition of high mobility group box 1 cytokine responsible for the activation of nuclear factor-κB pathway in atopic dermatitis. To evaluate the efficacy of resveratrol through topical route we have developed resveratrol-loaded nanoemulgel for the effective management of atopic dermatitis in mice model. The resveratrol-loaded nanoemulsion (0.5%, 0.75% and 1% w/w) was optimized by spontaneous nano-emulsification. The optimized resveratrol-loaded nanoemulsions showed average globule size in the 180-230nm range and found to be monodispersed. The resveratrol nanoemulgel was prepared with a SEPINEO™ P 600 gel base and propylene glycol. Ex vivo permeation and retention study resulted in significantly higher skin retention of resveratrol from resveratrol-loaded nanoemulgel than free resveratrol-loaded gel. Preclinical efficacy of resveratrol nanoemulgel displayed promising therapeutic outcomes where, western blotting of skin tissues disclosed a significant reduction in the relative expression of high mobility group box 1, the receptor for advanced glycation end products, toll-like receptor-4 and phosphorylated nuclear factor-κB. Further, real-time polymerase chain reaction also disclosed a significant reduction in pro-inflammatory cytokines such as thymic stromal lymphopoietin, interleukin-4, interleukin-13, interleukin-31, tumor necrosis factor-α and interleukin-6. The histopathological examination of skin sections showed improvement in the skin condition. Collectively, the findings from our study showcased the significant improvement in the atopic dermatitis skin condition in mice model after topical application of resveratrol loaded nanoemulgel.

Phage Delivery Strategies for Biocontrolling Human, Animal, and Plant Bacterial Infections: State of the Art.

This review aims at presenting the main strategies that are currently available for the delivery of bacteriophages to combat bacterial infections in humans, animals, and plants. It can be seen that the main routes for phage delivery are topical, oral, systemic, and airways for humans. In animals, the topical and oral routes are the most used. To combat infections in plant species, spraying the plant's phyllosphere or drenching the soil are the most commonly used methods. In both phage therapy and biocontrol using phages, very promising results have been obtained so far. However, more experiments are needed to establish forms of treatment and phage doses, among other parameters. Furthermore, in general, there is a lack of specific standards for the use of phages to combat bacterial infections.

Nanocrystals: A Multifaceted Regimen for Dermatological Ailments

AbstractSkin disorders are the most common apprehension worldwide among different regions of the world. Topical route of administration offers benefits over other routes such as avoidance of first‐pass metabolism, low dose, longer residence time, and absence of off‐target delivery. Skin serves as a mechanical barrier for therapeutic delivery with selectively permeable essential molecules. Considering the structural complexity of skin, delivery of therapeutics at targeted site requires sophisticated method such as nanotechnology‐assisted therapeutic delivery. The roadmap for combinatorial approach of nanotechnology and skin therapeutics has proven significant in clinical and marketed products. Currently, various pharmaceutical aids such as nanocrystal (NCs), nanoparticles, nanoemulsion, nano‐micelles, nano lipidic carriers, and hybrid nanocarriers are currently in market. Among all the other nanocarriers, nanocrystal offers precedence over other nanocarriers due to its facile method of preparation, reproducibility, low excipient concentration, and high therapeutic loading capacity. The recent literature data suggest the breakthrough evolution of NCs in topical therapeutic delivery. The outcome of these interventions envisages the applicability of NCs for delivering molecules with compromised physicochemical characteristics such as solubility, stability, toxicity, and bioavailability concerns.

A Review on Liquid Dosage Form

Liquid dosage forms are formulations that are administered through oral, parenteral and topical routes. Liquid dosage forms have better patient compliance as compared to other dosage forms hence, mainly used in paediatric patients. Also, during formulation the drugs are uniformly dispensed in liquid dosage form. It masks the taste of bitter, salty and nauseous drugs. This dosage form enhances the drug absorption and in turn, drug bioavailability. During formulation, some non-therapeutic agents (additives) are added that not have any pharmacological potential but still used to enhance the stability, appearance and efficacy of the dosage form to provide better compliance.

Nanostructured Lipid Carrier for Hyperpigmentation Treatment - a Dermal Prospective

The normal human skin is exposed to different types of infection like wrinkles, pigmentation, acne, pimples in which pigmentation is most common in women over 30-40 years. The field of nanotechnology is currently intensely exploited for drug delivery technology for passive and active targeting via various routes of administration, such things can be effectively treated by incorporating the drug, loaded in a Nanostructured lipid carrier (NLC). NLCs have shown potential in delivering poorly soluble active components and in depigmenting. NLC springs up as the second generation of lipid nanoparticles to overcome the shortcomings of first generation through the topical route. NLC in topical administration provides some added advantages like increasing skin hydration and modified release profile and increase in skin penetration leading to avoidance of systemic absorption. NLCs are composed of biocompatible lipids, surfactants, and cosurfactants which help enhance drug loading capacity and stabilize the formulation. NLC's remarkable physicochemical and subsequently biocompatible qualities have created an ongoing need for the development of beneficial and safe drug delivery methods. The key attributes of NLC that make them a promising drug delivery system are ease of preparation, biocompatibility, the feasibility of scale-up, non-toxicity, improved drug loading, and stability Their ingredients have a special impact on the end product's physicochemical characteristics and efficacy. The present review aims to focus on the recent advancement in the preparation, characterization, and applications of NLC in treating hyperpigmentation.

Assessment of the safety and efficacy of intravenous versus topical tranexamic acid in patients undergoing primary total hip and knee arthroplasty surgeries with respect to decreasing peri-operative blood loss and blood transfusion rates: a prospective and comparative study

Background: Synthetic antifibrinolytic agent like tranexamic acid has been increasingly used in Arthroplasty surgeries to decrease the peri-operative blood loss. The current study was undertaken to compare the efficacy between the intravenous and Topical route of TXA in deceasing the blood loss and transfusion rate in patients undergoing primary total hip and knee arthroplasty (THR and TKR) surgeries. Methods: A total of 120 patients were enrolled in the study with 60 each undergoing THR and TKR surgeries with 30 each given TXA in IV and Topical routes. Outcomes were assessed in terms of mean 24 hours drain output, mean blood loss, mean drop in hemoglobin blood transfusion rate. Results: The mean drain output was more in the IV group in both THR and TKR patients (p>0.05). The mean blood loss was more in the Topical group in both THR and TKR patients (p>0.05). The mean drop in hemoglobin was more in the Topical group, with the difference being significant in the THR patients (p<0.05) and being insignificant in TKR patients (p>0.05). In IV group 9 patients (15%) and in Topical group 25 patients (41.67%) needed blood transfusions, the difference being statistically significant. Conclusions: Both IV and Topical routes of TXA are equally effective in decreasing the peri-operative blood loss and transfusion rates in patients undergoing primary arthroplasty surgeries, with IV route having slightly upper hand as compared to the Topical route.

Six-Year Prescription Pattern of Antimicrobial Use in Cats at the Veterinary Teaching Hospital of the University of Pisa

The use of antimicrobials has greatly contributed to improving animal health. However, their inappropriate use reduces their effectiveness in treating bacterial infections and contributes to the selection of resistance. This study aimed to retrospectively evaluate the six-year pattern (2017–2022) of antimicrobial use in cats visiting the Veterinary Teaching Hospital (VTH) of the University of Pisa (Italy). The total number of prescribed antimicrobials, the number of animals for which an antimicrobial was prescribed, and the total number of antimicrobial prescriptions showed a significant time trend decrease during the study period, except for the fixed-dose combinations. The most frequently prescribed antimicrobials were amoxicillin-clavulanic acid (Synulox) (39.1%) followed by enrofloxacin (29.8%). These antimicrobials were mostly prescribed to treat infections affecting the genitourinary tract (~30%), followed by the gastrointestinal tract, skin, and respiratory system affections. Antimicrobials in empirical associations represented 13.0% of the total antimicrobial prescriptions, and the combination of amoxicillin-clavulanic acid (Synulox) with enrofloxacin accounted for the majority. The oral route represented the main route of administration of prescribed antimicrobials, followed by parenteral and topical ones. Amoxicillin-clavulanic acid (Synulox) (37.2%), ceftriaxone (2.7%), and tobramycin (2.8%) were the most prescribed antimicrobials for the oral, parenteral, and topical routes, respectively. Antimicrobial prescriptions complied with prudent use recommendations in terms of availability of diagnosis, respect to the dose range, duration of treatment, and the use of medicinal products approved for the species. On the contrary, antimicrobial susceptibility tests were used infrequently (5.2%), lacking compliance with the existing guidelines observed in companion animal practice. Overall, additional interventions are required not only to improve the responsible use of antimicrobials in our feline practice but also to implement antimicrobial stewardship programs, enhancing diagnostics such as culture and sensitivity testing in the future.

(334) Worldwide Interest in Testosterone Replacement Therapy

Abstract Introduction Testosterone therapy has gained popularity in recent decades, with various methods of administration available, such as oral, topical, injection, and implantable routes. As a wider variety of treatment options arise, knowledge regarding the public interest in varying modalities may give providers an insight to patient preferences and assist in the counseling of patients seeking to initiate testosterone replacement therapy. Objective To examine public interest in the different methods of testosterone administration across the United States and compare their relative popularity to intramuscular injections. Methods Utilizing Google Trends, data pertaining to searches related to diverse testosterone administration methods were collected over a ten-year duration. The categories under analysis encompassed 1) testosterone injections, 2) implanted testosterone, 3) oral testosterone, and 4) topical testosterone. Controlled search terms, including news and weather queries, were employed. Search term trends were quantified in arbitrary units (a.u.) and plotted against the corresponding time period. Results Testosterone injection had the highest average search intent from Google Trends during the past 10 years (63.08 +/- 12.7 a.u.), followed by testosterone pills (60.56 +/- 13.4 a.u.), testosterone pellets (53.14 +/- 19.4 a.u.), testosterone patches (51.03 +/- 16.2 a.u.), and lastly testosterone gel (17.29 +/- 21.5 a.u.) A notable upward trend was recorded for all searches, with the highest increase in searches seen for implanted testosterone (m = 0.433), testosterone injections (m = 0.297), oral testosterone (m = 0.222), and lastly topical testosterone (m = 0.050) (Figure 1). Conclusions This study provides compelling evidence that all modes of testosterone administration had increasing search trends, most notably implantable testosterone therapies followed by testosterone injections, and oral testosterone, which may be in line with recent FDA approvals since 2019 for newer oral (Jatenzo, Tlando, Kyzatrex) and implantable (ex: Xyosted) options. Disclosure Any of the authors act as a consultant, employee or shareholder of an industry for: Antares Pharma, Clarus Therapeutics, Coloplast.

Healing of diabetic foot ulcer with topical and oral administrations of herbal products: A systematic review and meta-analysis of randomized controlled trials.

This systematic review aimed to qualitatively synthesize recent randomized controlled trials (RCTs) regarding the effect of topical application and oral intake of herbal products on the healing of diabetic foot ulcer (DFU). Also, we sought to pool the obtained findings in a meta-analysis using a random-effects model, if RCTs were relatively comparable and homogenous. A comprehensive search was performed on five electronic data sources from their inception through 23 January 2024. The RCTs, without restriction on the country of origin, were included if they compared the effect of administering standard treatments and/or placebo (i.e. control condition) to applying standard treatments and/or herbal products in topical or oral routes (i.e. experimental condition). Out of 1166 retrieved records, 28 RCTs were included. Studies used different poly and single herbal formulations. Based on the meta-analysis, administration of standard care plus daily dressing of the ulcer site with olive oil for 28 days significantly increased the total ulcer healing score (3 RCTs; weighted mean difference [WMD] = 89.30; p < 0.001), raised frequency of complete ulcer healing (2 RCTs; risk ratio [RR] = 12.44; p = 0.039) and declined ulcer degree (3 RCTs; WMD = -22.28; p = 0.002). Also, daily use of the bitter melon leaf extract in oral form for 28 days significantly increased the total ulcer healing score (2 RCTs; WMD = 0.40; p = 0.001). Additionally, based on qualitative synthesis, the adjuvant use of herbal agents seems an intriguing choice to manage DFU. Nonetheless, considering the undesirable methodological quality of most studies and the high heterogeneity in administered herbal formulations, more robust trials are required to build a solid conclusion regarding the use of herbal products for healing DFU.

Topical tranexamic acid (TXA) is non-inferior to intravenous TXA in adult spine surgery: a meta-analysis.

Tranexamic acid (TXA) has long been utilized in spine surgery and can be administered through intravenous (IV)and topical routes. Although, topical and IV administration of TXA are both effective in decreasing blood loss during spine surgery, complications like deep vein thrombosis (DVT) and pulmonary embolism have been reported with the use of intravenous TXA (ivTXA). These potential complications may be mitigated through the use of topical TXA (tTXA). To assess optimal dosing protocols and efficacy of topical TXA in spine surgery, Embase, Ovid-MEDLINE, Scopus, Cochrane, and clinicaltrials.gov were queried for original research on the use of tTXA in adult patients undergoing spine surgery. Data parameters analyzed included blood loss, transfusion rate, thromboembolic, and other complications. Data was synthesized and confidence evaluated according to the Grades of Recommendation, Assessment, Development, and Evaluation approach. Nineteen studies were included in the final analysis with 2197 patients. Of the 18 published studies, 9 (50%) displayed high levels of evidence. Topical TXA showed a trend towards a lower risk of transfusion and complications. Protocols that used 1g tTXA showed a significantly reduced risk for transfusion when compared to controls (risk ratio -1.05, 95% CI (-1.62, -0.48); P = 0.94, I2 = 0%). Complications associated with tTXA included DVTs and wound infections. Topical TXA was non-inferior to intravenous TXA with similar efficacy and complication profiles for bleeding control in spine surgery; however, more studies are needed to discern benefits and risks.

In-Vitro and in-Vivo Evaluation of the Developed Curcumin-Cyclosporine-Loaded Nanoemulgel for the Management of Rheumatoid Arthritis

ABSTRACT Background Topical nanogel-based formulations have shown potential in the management of rheumatoid arthritis (RA). The aim of this research work was to explore the synergistic effect of Curcumin (CUR) and Cyclosporine (CYC) in combination via a topical route for the management of RA. Methods The CUR+CYC loaded nanoemulsion was developed using the spontaneous emulsification technique and was subsequently incorporated into Carbopol® Ultrez 30-NF gel. The effect of the developed formulation on levels of proinflammatory cytokines (IL-6, TNF-α) and anti-inflammatory cytokine (IL-10) was evaluated using lipopolysaccharide (LPS) induced RAW 264.7 cell culture model. The anti-arthritic activity was evaluated in a Complete Freund’s Adjuvant (CFA) induced arthritic rat model. Results The optimized nanoemulgel (CUR + CYC NE gel) exhibited average globule size of 15.32 nm ±2.7 nm, poly-dispersity index of 0.181 ± 0.034 and zeta potential of −16.3 mV ± 0.9 mV. The cumulative drug release from ex-vivo diffusion studies on porcine ear skin was 99.189% ± 1.419% at the of 24 h and 99.177% ± 1.234% at the end of 18 h for CUR and CYC, respectively. The cell culture studies revealed that the formulation was able to significantly lower (p < .001) the levels of IL-6 and TNF-α, inhibited prostaglandin E2 (PGE2) while significantly elevating (p < .001) the levels of anti-inflammatory cytokine (IL-10). The gel was found to be non-irritating and showed the inhibition of paw edema and substantial reduction of arthritic symptoms in an arthritic rat model as compared to commercial and other conventional alternatives. Conclusion This study highlights the potential of the developed nanoemulgel for the management of RA by enhancing the topical permeation of CUR and CYC.

Protein Nanoparticles Laden In situ Gel for Topical Ocular Drug Delivery.

Topical ocular delivery of drugs is most commonly preferred route by the patient and physician for the treatment of ocular diseases. The topical route is always followed with the disadvantages like tear turnover, nasolacrimal drainage, reduction in precorneal residence time, etc</i>. To overcome these hindrances associated with topical ocular route, a novel drug delivery system is used for targeting the drug at a specific site. In the Novel Drug delivery System, protein-based nanoparticles are an attractive class of nanoparticles designed to deliver the drug at targeted site in slow and sustained release manner. They have a size in the range of 1-100 nm. Protein nanoparticles are leading, particularly for the topical ocular delivery like reduction in intra ocular pressure, providing sustained release and targeted drug delivery at the site of its action. Various methods are used for formulation of protein nanoparticles like desolvation, emulsification, complex coacervation, electrospray techniques. The characterization parameters include particle size, surface morphology, drug loading and entrapment efficiency. Protein nanoparticles can also be loaded in to the in situ</i> gel forming polymers for increasing precorneal residence time of nanoparticles. The characterization parameters of in situ</i> gelling systems are gelling time, rheological properties, gel strength. The review mainly describes the use of various proteins in preparation of protein nanoparticles, methods for preparation of protein nanoparticles, polymers used in in situ</i> gelling system and evaluation as well as characterization parameters of protein nanoparticles, in situ</i> gelling systems & patented information related to protein nanoparticles and in situ</i> gelling system for ocular drug delivery.

Cationic-motif-modified exosomes for mRNA delivery to retinal photoreceptors.

Topical treatment of vitreoretinal diseases remains a challenge due to slow corneal uptake and systemic clearance. Exosomes are emerging nanocarriers for drug delivery due to biocompatibility and cellular targeting properties. To apply them for retinal targeting via the topical route, exosomes must traverse various ocular barriers including the cornea, lens, vitreous humor (VH), and the retina itself. Here we engineered high-purity milk-derived exosomes by anchoring arginine-rich cationic motifs via PEG2000 lipid insertion on their surface. Modification enabled exosomes to use weak-reversible electrostatic interactions with anionic glycosaminoglycan (GAG) and water content of the tissue to enhance their transport rate and retention. Addition of cationic motifs neutralized the anionic surface charge of exosomes (-24 to -2 mV) without impacting size or morphology. Cationic-motif-modified exosomes exhibited two-fold faster steady state diffusivity through bovine corneas compared to unmodified exosomes. Fluorescence recovery after photobleaching confirmed that cationic-motif-modified exosomes can diffuse through VH without steric hindrance. In healthy VH, cationic-motif-modified exosomes demonstrated stronger binding resulting in three-fold lower average diffusivity that enhanced by six-fold in 50% GAG-depleted VH recapitulating advanced liquefaction. Cationic-motif-modified exosomes penetrated through the full-thickness of porcine retinal explants resulting in ten-fold higher uptake in photoreceptors and three-fold greater transfection with encapsulated eGFP mRNA compared to unmodified exosomes. Cationic-motif-modified exosomes are safe to use as they did not adversely affect the mechanical swelling properties of the cornea or lens nor impact retinal cell viability. Cationic-motif-modified exosomes, therefore, offer themselves as a cell-free nanocarrier platform for gene delivery to retinal photoreceptors potentially via the topical route.

Study of prescription pattern of antifungal drugs from tertiary care hospital

Background: The most common superficial fungal infections are tinea corporis, tinea cruris, tinea capitis, tinea pedis, tinea unguium, and tinea facie and cutaneous Candida albicans infections such as oral thrush, oropharyngeal candidiasis, vaginal candidiasis, and onychomycosis. Aims and Objectives: (i) Analysis of prescription pattern of antifungal drugs and (ii) to study common adverse effects. Materials and Methods: A retrospective, observational study conducted in B. K. L. Walawalkar Hospital, Sawarde, Ratnagiri. A total of 993 case papers were analyzed after getting approval from the institutional ethics committee and permission from dermatology department. The frequency with percentage was used for the analysis of data. Results: In 993 patients with superficial fungal infections, 523 (52.7%) were males and 470 (47.3%) were females. Majority of patients were belonged to 21–40-year age group, i.e., 439 (44.2%) followed by 41–60 years, i.e., 244 (24.6%). Our study shows that the most common superficial fungal infections with single lesion were tinea corporis (22.3%), tinea cruris (14.6%), and pityriasis versicolor (13.9%). In Candida albicans, the most common infection was onychomycosis 14 (1.4%). The most common antifungal prescribed was luliconazole (20.84%) followed by itraconazole (20.58%). The most common route was topical route (68.26%). Combination of drugs was not prescribed. Different prescription indicators were that the average number of drugs prescribed per encounter was 3.4 and average number of drugs prescribed per encounter was 2.7. Conclusion: Most commonly prescribed newer antifungal was luliconazole. Next most commonly prescribed by oral route was itraconazole. No use of combination of drugs and many drugs selected from essential medicinal list. Based on these finding we concluded prescriptions where rational approach.

Preparation and Evaluation of Diclofenac Sodium Loaded Liposomal Hydrogel in the Treatment of Rheumatoid Arthritis

In the present research, it was proposed to provide topical delivery of diclofenac sodium. Diclofenac sodium will be encapsulate in liposome and further loaded into a hydrogel and delivered through topical route. The lipid film hydration approach was used to create diclofenac sodium liposomes, which were then characterised by vesicle size, zeta potential, and entrapment effectiveness. The pH of the generated liposomal gels was within the permissible range of 7.0-7.2. The spreadability of the gels was assessed using slip and drag characteristics and was found to be between 10.45 and 12.32 gm.cm/sec. F1, F2, and F3 spreadabilities were determined to be 10.45±0.075,12.32±0.042 and 11.75±0.049 gm.cm/sec, respectively. The viscosities for F1, F2, and F3 were determined to be 1870±25 cps, 1895±33 cps, and 1875±21 cps, respectively. The percentage of cumulative medication (diclofenac sodium) released from F1, F2, and F3 liposomal gel formulations was 98.15%±17, 98.72%±2.4 and 96.27%±2.7 respectively.

Quality by Design Assisted Development of Luliconazole Transethosomes in Gel for the Management of Candida albicans Infection.

The objective of this study was to develop and evaluate a novel vesicular formulation of luliconazole (LUL) for the management of Candida albicans infection through a topical route. LUL-loaded transethosomes (LUL-TE) were prepared by the film hydration method and various independent and dependent variables were optimized using the Box-Behnken design. Selected critical material attributes were the content of phospholipids (X1), concentration of ethanol (X2), and amount of sodium cholate (X3). Formulated LUL-TE were characterized for percent entrapment efficiency, percent drug loading, vesicle size, and polydispersity index (PDI) and were incorporated into the carbomer gel base and further evaluated for gel characterizations. The prepared transethosomal gel (LUL-TE-CHG) was evaluated for pH, spreadability, viscosity, antifungal activity, and in vitro study. From the observed results, it was evident that the prepared LUL-TE-CHG was in the desired pH (6.2 ± 0.45), spreadability [8.3 ± 0.42 g/(cm·s)], viscosity (236.1-19.2.26 mPa·s), nanovesicle size (252 ± 9.82), entrapment efficiency (85% ± 5.24%), zeta potential (-34.05 ± 3.52 mV), and PDI (0.233 ± 0.002). The zone of inhibition results suggested that the LUL-TE-CHG formulation has the highest antifungal activity, that is, 5.83 ± 0.15 mm3. The in vitro results showed that drug release within 2 h was 18.1% ± 2.0% and after that sustained release action, 83.2% ± 1.7% within 8 h. Finally, to confirm the therapeutic efficacy of the developed formulation, fungal infection was induced by using C. albicans in Wistar rats. In vivo, skin irritation study and histopathology studies were performed in the disease-induced model. Animal experiments revealed that LUL-TE-CHG has significantly improved the diseased condition in Wistar rats. The results observed from the skin permeation and skin deposition profile ensure that the prepared novel LUL-loaded TE system had a higher permeation rate and increased retention time compared with LUL-CHG. The hydrogel incorporated with LUL could be a novel approach with safe and effective fungal treatment.

Drug utilization pattern evaluation and cost variation analysis of anti-fungal agents in tinea infected patients in dermatology department of a tertiary care teaching hospital

Background: Tinea infections are chronic superficial fungal infections, highly prevalent in tropical countries like India. Therefore, long-term therapy is needed and this can inflict a financial burden on the patients. Aim of the study was to assess drug utilization patterns in patients diagnosed with tinea infection and to evaluate the cost variability of anti-fungal agents. Methods: A cross-sectional observational study was conducted in patients for 3 months after taking permission from IEC. All adult patients already diagnosed with tinea infection were enrolled. Evaluation of drug utilization pattern was carried out using WHO core drug prescribing indicators and percentage of cost variability was calculated between different brands of anti-fungal agents. Results: A total of 252 patients were enrolled. Tinea corporis and cruris were the most commonly diagnosed tinea infection. Pruritus was the most common presenting symptom. Past history of similar illness was seen in 74 (29.4%) patients mean of 3.83±0.87 drugs were prescribed per patient. Drugs prescribed from NLEM was only 42.1%. Most commonly prescribed drugs were oral itraconazole and topical miconazole. Percentage of cost variability was seen maximum with capsule itraconazole 200 mg (237.5%) by oral route and luliconazole 30 gm (175.6%) by topical route. Conclusions: Prescribing practices of drugs can be improved by promoting generic drug and prescribing drugs from NLEM. Wide range of cost variation can lead to high economic burden in tinea infected patients.

Microemulgel Delivery of Ciprofloxacin Hydrochloride

Background: Ciprofloxacin hydrochloride is broad spectrum carboxyfluoroquinolone antibiotic from biopharmaceutics classification system (BCS) class IV. The oral dosage form exhibits gastric irritation whereas the topical cream has demonstrated poor penetration and low bioavailability. Objective: To optimize microemulsion-based gel of ciprofloxacin hydrochloride to increase its solubility and permeability through the cutaneous layer for targeting bacterial skin infections. Methods: To develop microemulsion, oil (soya oil, castor oil, oleic acid, isopropyl myristate and vegetable oil), surfactant (cremophore, span 80, tween 80) and cosurfactant (PEG 600 and PEG 400, propylene glycol) were evaluated. To depict the microemulsion formulation pseudo ternary phase diagram was employed. %Transmittance, zeta potential, dissolution study and size analysis were carried out for evaluation of microemulsion. 32 factorial design was used. Two variables i.e concentration of Sepineo P600 and Carbopol 934 effect on microemulgel was evaluated. Evaluation of gel was carried for physical parameters, antimicrobial, in-vitro and ex-vivo release study. Results: Solubility analysis suggested tween 80, oleic acid and propylene glycol for the formulation of microemulsion. Zeta potential for microemulsion batch F1 was -11.3 mV. This indicated good stability. In-vitro release study showed 91.98% percentage cumulative drug release for batch F1 at 8 hours. Microemulsion-based gel (F1) showed 22.96% inhibition against bacteria which proved its antibacterial activity. Conclusion: The obtained results exhibited that the permeability and bioavailability of the drug was increased when given through a topical route.

Nanosponges- A Versatile Approach of Drug Delivery System

With the escalating number of diseases, an opportunistic target drug delivery system is needed. Nanosponges (NS) are nanosized drug delivery systems having three-dimensional (3D) configurations, fabricated by crosslinking of polymers to ensnare a wide assortment of drugs. These small particles move inside the body till they arrive at the target site and deliver the medication in a specific and controlled way. They can ensnare (entrap) both hydrophilic and hydrophobic moieties in a smarter manner and improve the solubility and bioavailability of drugs. NS have been utilized to examine the medication conveyance by oral, parenteral, and topical routes. Another significant property of NS is that they can work on the solvency of ineffectively water-soluble moieties and are utilized for the storage of gases, and proteins as well as for the removal of toxins from the systemic circulation. The present review highlights the types of nanosponges, their methods of preparation, characterization, and applications in drug delivery.