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 Table of Contents  
ORIGINAL/BRIEF
Year : 2012  |  Volume : 4  |  Issue : 5  |  Page : 74-76  

Preliminary investigation tests of novel antifungal topical aerosol


Babaria Institute of Pharmacy, Varnama, Vadodara, Gujarat, India

Date of Web Publication21-Mar-2012

Correspondence Address:
M Monali Kapadia
Babaria Institute of Pharmacy, Varnama, Vadodara, Gujarat
India
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/0975-7406.94145

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   Abstract 

Spray formulation can minimize pain and irritation experience during the application of conventional dosage forms. Econazole Nitrate is an active ingredient of the aerosol concentrate to be used for twice-daily application because of its long durability in the superficial layers of the fungal infected skin. The aim of this study is preliminary investigation of Econazole Nitrate spray by varying the concentrations of different constituents of the spray. The ratios of Propylene glycol (PG) and isopropyl myristate (IPM) were selected as independent variables in 2 2 full factorial designs, keeping the concentration of solvent, co-solvent and propellant LPG constant. Aerosol also contained Ethanol as solvent and Isopropyl alcohol as co-solvent. All ingredients of the aerosol were packaged in an aluminum container fitted with continuous-spray valves. Physical properties evaluated for the Econazole Nitrate spray included delivery rate, delivery amount, pressure, minimum fill, leakage, flammability, spray patterns, particle image and plume angle. Glass containers were used to study incompatibility between concentrate and propellant due to the ease of visible inspection. Isopropyl myristate at lower concentrate showed turbidity, while at high concentration it met the requirements for aerosol and produced Econazole Nitrate spray with expected characteristics.

Keywords: Topical spray, delivery rate, minimum fill, plume angle


How to cite this article:
Kapadia M M, Solanki S T, Parmar V, Thosar M M, Pancholi S S. Preliminary investigation tests of novel antifungal topical aerosol. J Pharm Bioall Sci 2012;4, Suppl S1:74-6

How to cite this URL:
Kapadia M M, Solanki S T, Parmar V, Thosar M M, Pancholi S S. Preliminary investigation tests of novel antifungal topical aerosol. J Pharm Bioall Sci [serial online] 2012 [cited 2020 Sep 24];4, Suppl S1:74-6. Available from: http://www.jpbsonline.org/text.asp?2012/4/5/74/94145

Skin diseases are usually visible and accessible. This means that the majority of skin diseases including fungal infection may be treated topically with treatment delivered directly to the desired site of action, thereby avoiding, or at least we hope attenuating, the potential for systemic side effects. Among the skin disorders, fungal infections that affect the skin and adjacent structures are common in all environments. Many widely used topical formulations like ointments, creams, gels; lotions have some limitations in the application and maintenance processes. To overcome the limitations of the conventional dosage forms, spray or aerosol dosage form for topical application have been formulated. Econazole Nitrate a broad spectrum antimycotic agent is widely used as superficial antifungal agent is selected as model drug candidate to formulate antifungal topical spray. The topical spray dosage form is indented to deliver the bioactive compound directly to the infected area and produce a film that covers infection which acts as reservoir for the bioactive drug. Econazole Topical pharmaceutical aerosols offers aesthetic properties, ease of application, and maintainability of integrity, tamperproof system and prevention of contamination of the unused contents. The objective of this study is to carry our preliminary investigation of Econazole Nitrate spray. [1]


   Materials and Methods Top


Econazole Nitrate was obtained as gift sample from J. B Chemicals and pharmaceuticals Ltd, Ankleshwar Gujarat. Ethanol and Isopropyl alcohol were Procured in house, Isopropyl microstate and Propylene glycols were purchased from colichem. Aerosol canisters along with valve assembly and LPG Propellant were provided by Vimsons Aerosols, Anand, and Gujarat.

Econazole Nitrate (1%) was dissolved in Ethanol (25%) and Isopropyl Alcohol (5%). Isopropyl microstate was added in two different concentrations i.e., 2.5% and 5% for different formulations. Similarly, Propylene glycol was added in two different concentrations i.e., 5% and 10% for different formulations. The solutions were than stirred for 10 minutes with the help of glass rod. Approximately 20 ml of solution was filled in to each of 50 ml aluminum aerosol canisters. The valve was placed and sealed to the canister before filling the propellant manually by using aerosol filling machine. The density of propellant was 0.55 g/ml and weight of propellant filled in the container was 11 g. The canisters were shaken and the Econazole Nitrate sprays were prepared for further evaluations for Physical compatibility of aerosol concentrates with propellants, Delivery rate, Delivery amount, Pressure test, Minimum fill, Flammability, Spray patterns, Particles size and particles image, Spray angle.


   Results and Discussion Top


Compatibility of aerosol concentrates with propellants

Glass containers were used in this study to observe any change taking place visually which reflect the compatibility of the formulated aerosol. Drug concentrate was found to be clear at higher concentration of Isopropyl microstate and showed turbidity at lower concentration which was undesired for the further studies. [2]

Delivery rate and delivery amount of the Econazole Nitrate formulated spray

Delivery rate and delivery amount of Econazole Nitrate spray formulated are shown in [Table 1]. The delivery rate of Econazole Nitrate spray was found to be almost same for all the formulations. The delivery amount was found to be less for formulations with lower concentration of Isopropyl microstate. [2],[3]
Table 1: Delivery rate and delivery amount of Econazole Nitrate at different concentrations of IPM and propylene glycol in formulation F1-F4, Mean±SD, (n=6)

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Minimum fill of the formulated Econazole Nitrate spray

All formula had a minimum fill of more than 100%, which mean that the net weight of the contents was not less than the labelled amount and met the requirement [ 3] and presented in [Table 2].
Table 2: Minimum fill and flammability test of Econazole Nitrate spray Mean±SD, (n=12)

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Flammability of the formulated Econazole Nitrate spray [2]

The results of flammability test are shown in [Table 2].

Spray pattern of the formulated Econazole Nitrate spray [2],[3]

The results of spray pattern of Econazole Nitrate spray are shown in [Figure 1]. The patterns and size were almost the same since all formula used the same type of valve. It means that spray patterns were not significantly affected by different concentrations of IPM and Propylene glycol. The type of valve used might affect the spray pattern.
Figure 1: Spray pattern of Econazole Nitrate spray

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Particle size and particle image of formulated Econazole Nitrate spray [2]

The particles size and particles image of Econazole Nitrate spray are shown in [Figure 2] and [Figure 3], [Figure 4]. Particles size and particles image of Econazole Nitrate spray using LPG propellant were found almost same.
Figure 2: Particle image of Econazole Nitrate spray

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Figure 3: Particle size of Econazole Nitrate spray

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Figure 4: Spary angle

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Spray angle [2]

Spray angle was found to be 19° according plume geometry for all formulations.


   Discussion Top


Preliminary investigations evaluating product performance test proved that the formulation F3 having equal percentage of IPM and PG is stable and chemically and physically compatible having low delivery rate comparing to F1, F2 and F4. Delivery amount determined for F3 is maximum showing uniformity of solution while for F1, F2 and F4 is low. Spray pattern for all formulations was spherical and mean particle size for F3 was spherical spray pattern and mean particle size was 6.35 μ. Spray angle was narrow allowing point application of drug to affected part. None of the canister was found leaked and minimum fill volume was optimum for F3 also flame projection and flame back was according to requirement.


   Conclusions Top


Preliminary investigation study of the econazole nitrate topical aerosol suggest LPG is suitable propellent. Further the physiochemical and product performance tests proved the econazole nitrate topical spray would be a convenient delivery for superficial fungal infections. Invitro diffusion and antifungal activity evaluation will establish the efficacy of econazole nitrate topical aerosol delivery.


   Acknowledgments Top


This study was supported by Vimson Aerosols, Anand, Gujarat.

 
   References Top

1.Fromtling R, Overview of Medically Important Antifungal Azole Derivatives. Clinical Microbiology Reviews, Apr.1988;2: Pg no. 187-217.  Back to cited text no. 1
    
2.Lachman L, Lieberman HA, Kanig JC, The Theory and Practice of Industrial Pharmacy, Varghese Publishing House, Bombay, 1991; 589-618.  Back to cited text no. 2
    
3.USP, Physical test and Determination, in United States Pharmacopoeia. United States Pharmacopeial Convention: Rockville. 2000; 1895-96.  Back to cited text no. 3
    


    Figures

  [Figure 1], [Figure 2], [Figure 3], [Figure 4]
 
 
    Tables

  [Table 1], [Table 2]


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