scholarly journals Antifungal Topical Nanoemulgel Containing Miconazole Nitrate

2021 ◽  
Vol 11 (11) ◽  
pp. 208-229
Author(s):  
Anju K P ◽  
Shripathy D ◽  
Shabaraya A R

Nanomulgel have emerged as one of the most interesting topical drug delivery system as it has dual release control system i.e. nanoemulsion and gel. Also the stability of nanoemulsion is increased when it is incorporated in gel. Miconazole nitrate is an antifungal medication topically administered to treat skin infections such as athlete’s foot, jock itch and ringworm. The aim of the present research work was to investigate the potential of nanoemulgel in enhancing the topical delivery of hydrophobic drug. MCZ nanoemulsions were prepared using span 80, tween 80, propylene glycol and different conc. of sunflower oil by High pressure homogenization technique. The prepared nanoemulsions were evaluated for pH, drug content, centrifugation, globule size and zeta potential.F2 showed highest drug content 91.26%.The globule size are found to be satisfactory range of nanoemulsion. The drug release kinetics is in the order of F2>F3>F4>F5>F1.And Nanoemulgel is prepared by using Carbopol 934 as gelling agent The release kinetics of nanoemulgel was found to obey zero order kinetics. The nanoemulgel was found to be stable with respect to physical appearance, pH, rheological properties spreadability and drug content at all temperature and conditions for two month. Hence, in the present study it can be concluded that Miconazole Nitrate nanoemulgel formulation is a promising system for the topical drug delivery and also an alternative method to deliver the hydrophobic drugs in water soluble gel bases. Key words: Hydrophobic drugs, Nanoemulgel, Miconazole nitrate, Topical drug delivery.

2017 ◽  
Vol 5 (01) ◽  
pp. 25-33 ◽  
Author(s):  
Shailendra Kumar Sah ◽  
Ashutosh Badola ◽  
Bipin Kumar Nayak

Topical drug delivery is mostly culled for the local dermatological action, but recently the new technologies are also enhancing its systemic effect. They are generally applied for the purpose as antiseptics, antifungal agents, skin emollients, and protectants. The activity of topical preparation confide in the various factors as drug solubility, its lipophilicity, contact time to skin, its permeability. Many widely used topical agents like ointments, creams, lotions, gel are associated with disadvantages like stability problems, stickiness and lesser spreading coefficient, irritation, allergic reactions, poor permeability, poor absorption and difficulty in absorption of large molecule, to rectify this the new concept of Emulgel has been introduced with the main objective to deliver hydrophobic drug molecule. Emulgel is oil in water or water in oil emulsion carrying drug to be incorporated in gel base to obtain gellified emulsion. Emulgel shows the controlled and better release effect of drug by virtue of combined effect of gel and emulsion with increased stability. Gel having various advantages as non greasy and favors good patient compliance in field of cosmetology and dermatology but are still limited to the deliver hydrophobic drugs. So the Emulgel comes to favour the hydrophobic drugs to give the advantages of gel. Emulgels have several advantages in the field of dermatology such as being thixotropic, greaseless, easily spreadable, easily removable, emollient, nonstaining, long shelf life, bio-friendly, transparent and pleasing appearance. Factors such as gelling agent, oil agent, emulsifiers influence the stability and efficacy of emulgel. So emulgels can be the better semisolid preparation than other conventional systems. At present the emulgel are being used for the delivery of analgesics, anti-inflammatory, anti-fungal, anti-acne drugs and various cosmetic formulations with still wide range to explore.


1970 ◽  
Vol 1 (3) ◽  
pp. 43-49 ◽  
Author(s):  
Jovita Kanoujia ◽  
Kanchan Sonker ◽  
Manisha Pandey ◽  
Koshy M Kymonil ◽  
Shubhini A Saraf

The present research work deals with the formulation and evaluation of in-situ gelling system based on sol-to-gel transition for ophthalmic delivery of an antibacterial agent gatifloxacin, to overcome the problems of poor bioavailability and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Carbopol 940 was used as the gelling agent in combination with HPMC and HPMC K15M which acted as a viscosity enhancing agent. The prepared formulations were evaluated for pH, clarity, drug content, gelling capacity, bioadhesive strength and in-vitro drug release. In-vitro drug release data of optimized formulation (F12) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. The clarity, pH, viscosity and drug content of the developed formulations were found in range 6.0-6.8, 10-570cps, 82-98% respectively. The gel provided sustained drug release over an 8 hour period. The developed formulation can be used as an in-situ gelling vehicle to enhance ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance. Key Words: In-situ gelation; Gatifloxacin; Carbopol 940; HPMC K15M. DOI: http://dx.doi.org/10.3329/icpj.v1i3.9661 International Current Pharmaceutical Journal 2012, 1(3): 43-49


Author(s):  
SHANKHADIP NANDI

3D printing technology is a rapid prototyping process based on computer-aided design software that is proficient to construct solid objects with various geometrics by depositing numerous layers in a sequence. The major advantages of three-dimensional printing (3DP) technology over the traditional manufacturing of pharmaceuticals include the customization of medications with individually adjusted doses, on-demand tailored manufacturing, unprecedented flexibility in the design, manufacturing of complex and sophisticated solid dosage forms, and economic benefits. Recently, many researchers have been invested their efforts in applying 3DP technology to the pharmaceutical development of drug products and different drug delivery systems. Selective laser sintering, fused deposition modeling, semi-solid extrusion, stereolithography, etc., are the multiple 3DP technologies that can be established in several customized and programmable medicines. Sublingual, orodispersible, and fast-dissolving drug delivery formulations by 3DP technology have been already manufactured. Controlled-release formulations with different characteristics, doughnut-shaped multi-layered tablets with linear release kinetics, and drug-loaded tablets with modified-release characteristics are recently fabricated using 3DP. However, few 3DP methods produce uneven shapes of dosage forms and comparatively porous structures. Cost of transition, adaptation to the existing facility, achieving regulatory approval, etc., are the present challenges that can restrict the extensive application of 3DP technology to pharmaceutical products. Intense research work for modifying the 3DP methods is simultaneously sustained for by-passing the flaws and current limitations of this technology. 3DP technology can act as a convenient and potential tool for the pharmaceutical industry which will set a revolutionary manufacturing style in the near future to facilitate patient-centered health care.


2012 ◽  
Vol 1 (12) ◽  
pp. 414-419 ◽  
Author(s):  
Durgacharan Arun Bhagwat ◽  
John Intru D’Souza

Improvement of bio-availability of poorly water soluble drugs presents one of the furthermost challenge in drug formulations. One of the most admired and commercially viable formulation approach for this challenge is solid self micro emulsifying drug delivery system (S-SMEDDS). There are many techniques to convert liquid SMEDDS to solid, but an adsorption technique is simple and economic. Hence aim of present study was to develop S-SMEDDS of poorly water soluble drug Telmisartan (TEL) using Aerosil 200 as solid carrier. Liquid SMEDDS was prepared using Acrysol EL 135, Tween 80 and PEG 400 as oil, surfactant and co-surfactant and was converted to S-SMEDDS by adsorbing it on Aerosil 200. Prepared S-SMEDDS was evaluated for flow properties, drug content, reconstitution properties, DSC, SEM, in-vitro drug release and ex-vivo intestinal permeability study. Results showed that prepared S-SMEDDS have good flow property with 99.45 ± 0.02% drug content. Dilution study by visual observation showed that there was spontaneous micro emulsification and no sign of phase separation. Droplet size was found to be 0.34 µm with polydispersity index of 0.25. DSC thermogram showed that crystallization of TEL was inhibited. SEM photograph showed smooth surface of S-SMEDDS with less aggregation. Drug releases from S- SMEDDS were found to be significantly higher as compared with that of plain TEL. Ex-vivo intestinal permeability study revealed that diffusion of drug was significantly higher from S-SMEDDS than that of suspension of plain TEL. Study concluded that S-SMEDDS can effectively formulated by adsorption technique with enhanced dissolution rate and concomitantly bioavailability.DOI: http://dx.doi.org/10.3329/icpj.v1i12.12451 International Current Pharmaceutical Journal 2012, 1(12): 414-419


Author(s):  
SACHIN SAGGAR ◽  
ASHUTOSH UPADHAYAY ◽  
MANISH GOSWAMI

Objective: The self-micro-emulsifying drug delivery system (SMEDDS) of bambuterol hydrochloride was designed, prepared, and evaluated to overcome the problem of poor bioavailability. Methods: The designing of the formulation included the selection of oil phase, surfactant, and cosolvent/cosurfactant based on the saturated solubility studies. Psuedoternary phase diagram was constructed using aqueous titration method, to identify the self-emulsifying region. Different ratios of the selected surfactant and cosolvent/cosurfactant (Smix) were also studied and used to construct the ternary phase diagram. The prepared formulations of the SMEDDS were evaluated for drug content, morphology, globule size, robustness to dilution, emulsification time, optical clarity, and stability. Results: The formulation containing 10 mg bambuterol hydrochloride, triacetin (12.50% w/w), Tween 80 (43.75% w/w), and ethanol (43.75% w/w) was concluded to be optimized. The optimized SMEDDS not only showed optimum globule size, zeta potential, and drug content but was also found to be robust to dilution, formed emulsion spontaneously, and was stable. The optimized SMEDDS showed increased permeability of the drug across the intestinal membrane in ex vivo studies. Conclusion: The results suggest that bambuterol hydrochloride can be formulated as self-microemulsifying drug delivery system, and further, SMEDDS can be used to improve the oral bioavailability of bambuterol hydrochloride.


Author(s):  
N. V. SAI PRIYANKA ◽  
P. NEERAJA ◽  
T. MANGILAL ◽  
M. RAVI KUMAR

Objective: The main objective of the present research work was to formulate and evaluate gel loaded with microspheres of apremilast to increase bioavailability and to reduce the dosing frequency and to improve patient compliance. Methods: Gel loaded with microspheres of apremilast was prepared by solvent evaporation method by taking different ratios of polymers. Ethyl cellulose as a polymer, dichloromethane solvent is used as drug solubility, polyvinyl alcohol as a surfactant, and sodium alginate is used as gelling agent. Prepared gel loaded with microspheres was evaluated for drug interactions by Fourier transform infrared (FTIR), differential scanning calorimetry studies, and surface morphology by scanning electron microscopy (SEM), to select effective one among all formulations. The prepared formulations (F1–F6) were evaluated for pre-formulation studies, spreadability, viscosity, pH measurement, gel strength, homogeneity, drug content, in vitro diffusion studies, drug kinetics, and finally for stability studies. Results: Differential scanning calorimeter studies confirmed that there is no drug interaction between drug and excipients. FTIR spectroscopy studies confirmed that there is compatibility between drug and excipients. Regular and spherical shape particles with smooth surface were observed in the SEM photographs. The optimized gel loaded with microspheres of F4 formulation (drug: polymer in 1:4 ratio) is more effective compared to all formulations. The prepared gel showed acceptable physical properties such as spreadability (5.86±0.54 g.cm/s), viscosity (568 cps), pH (6.33±0.55), gel strength (38 s) and drug content (90.00±0.71%). In vitro diffusion studies have shown 80.1±1.92% drug release in 10 h. Drug kinetics follows zero order kinetics and n value was found to be 0.721. Stability studies were done for 3 months. Conclusion: All the results show that the gel loaded with microspheres of apremilast can be effectively used for the treatment of psoriasis and psoriatic arthritis.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 209 ◽  
Author(s):  
Ajeesh Chandrasekharan ◽  
Young Jun Hwang ◽  
Keum-Yong Seong ◽  
Samdae Park ◽  
Sodam Kim ◽  
...  

Chitosan has been widely used as a nature-derived polymeric biomaterial due to its high biocompatibility and abundance. However, poor solubility in aqueous solutions of neutral pH and multiple fabrication steps for the molding process limit its application to microneedle technology as a drug delivery carrier. Here, we present a facile method to prepare water-soluble chitosan and its application for sustained transdermal drug delivery. The water-soluble chitosan was prepared by acid hydrolysis using trifluoroacetic acid followed by dialysis in 0.1 M NaCl solutions. We successfully fabricated bullet-shaped microneedle (MN) arrays by the single molding process with neutral aqueous chitosan solutions (pH 6.0). The chitosan MN showed sufficient mechanical properties for skin insertion and, interestingly, exhibited slow dissolving behavior in wet conditions, possibly resulting from a physical crosslinking of chitosan chains. Chitosan MN patches loading rhodamine B, a model hydrophilic drug, showed prolonged release kinetics in the course of the dissolving process for more than 72 h and they were found to be biocompatible to use. Since the water-soluble chitosan can be used for MN fabrication in the mild conditions (neutral pH and 25 °C) required for the loading of bioactive agents such as proteins and achieve a prolonged release, this biocompatible chitosan MN would be suitable for sustained transdermal drug delivery of a diverse range of drugs.


Author(s):  
Ajit Kulkarni ◽  
Suhit Gildai ◽  
Nagesh Alurkar ◽  
Rohit Bhosale ◽  
Riyaz Osmani

The present research work was carried out to develop novel drug delivery system i.e. temperature-sensitive gel containing propolis for mastitis. Mastitis is an inflammatory disease of mammary gland caused by bacteria, especially Staphylococcus aureus and its toxins. For this study, propolis was used as a drug or active agent to defeat the side effects associated with an antibiotic treatment and pluronic F127 (poloxamer 407) was used a gelling agent. Polymer solution was prepared by cold method and on the basis of gelation temperature and viscosity of polymer gel three batches having polymer concentration 18%, 19% and 20% were optimized and selected. Drug extract solution was then added in three optimized batches of polymer solution and final formulation was developed. After addition of solution containing drug extract in polymer solution, final formulation was studied for various parameters and it was found that gel forming ability of polymer solution was unaltered. Even after sterilization, the gel forming ability of formulation was unchanged which helped to select suitable method of sterilization for developed formulation. On the basis of data collected from various evaluation parameters, it was found that developed formulation offered a suitable and novel vehicle for drug delivery.


2020 ◽  
Vol 26 (2) ◽  
pp. 279-291
Author(s):  
Gururaj C. Aithal ◽  
Reema Narayan ◽  
Usha Y. Nayak

Recently, the delivery of hydrophobic/ poorly water-soluble drugs has been a challenging task. Various strategies have been developed to counter the former along with other prime issues, such as stability, bioavailability etc. However, only few formulations have been successful in addressing the problems and nanoemulgel is a standout among them. Nanoemulgels are appropriate candidates for drug delivery because of their dual character i.e. the presence of an emulsion in the nano scale and a gel base, both combined as a single formulation. The nanoemulsion component of the nanoemulgel conforms protection to the active moiety by preventing the enzymatic degradation and certain reactions like hydrolysis. The gel base attributes thermodynamic stability to the emulsion by increasing the viscosity of the aqueous phase by decreasing the interfacial and surface tension. Nanoemulgels possess rheological characteristics which are suited especially for topical delivery and other forms such as dental delivery with the aid of better patient acceptance. As the globule size is present in the nano form alongside the employment of certain penetration enhancers can increase the effectiveness of the formulation by enhancing the permeability and diffusibility. Reports suggest that certain commercially available topical dosage forms have a low spreading coefficient in comparison with the nanoemulgel thereby focusing on the application of nanoemulgels in the field of dermatology, although paving way for various other fields have not been thoroughly exploited. This comprehensive review highlights the benefits of nanoemulgel as a potential carrier for drug delivery with an overview of few illustrations supporting the cause.


2021 ◽  
Vol 903 ◽  
pp. 3-8
Author(s):  
Mārīte Skrinda ◽  
Arita Dubnika ◽  
Janis Locs

Liposomes are being used as unique drug delivery systems due to their ability to encapsulate both hydrophilic and hydrophobic drugs, as well as for the fact that they improve the disadvantages of free drug administration. However, liposomes have a significant disadvantage - low encapsulation efficiency. In the research carried out, 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) and cholesterol (Chol), in the ratio (n/n) of 2:1, 3:1 and 4:1 respectively, were used to prepare the liposomes. Blank liposomes (LIP) and vancomycin hydrochloride (VANKA) containing liposomes (VANKA-LIP) were prepared for each of the DSPC and Chol compositions. The aim of our study was to evaluate the effect of liposome composition on the VANKA encapsulation efficiency and release kinetics.


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