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ORIGINAL/BRIEF
Year : 2012  |  Volume : 4  |  Issue : 5  |  Page : 81-83  

Formulation and kinetic modeling of curcumin loaded intranasal mucoadhesive microemulsion


Parul Institute of Pharmacy, Limda, Vadodara, India

Date of Web Publication21-Mar-2012

Correspondence Address:
B Mikesh Patel
Parul Institute of Pharmacy, Limda, Vadodara
India
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Source of Support: None, Conflict of Interest: None


DOI: 10.4103/0975-7406.94148

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   Abstract 

It is a challenge to develop the optimum dosage form of poorly water-soluble drugs and to target them due to limited bioavailability, intra and inter subject variability. In this investigation, mucoadhesive microemulsion of curcumin was developed by water titration method taking biocompatible components for intranasal delivery and was characterized. Nasal ciliotoxicity studies were carried out using excised sheep nasal mucosa. in vitro release studies of formulations and PDS were performed. Labrafil M 1944 CS based microemulsion was transparent, stable and nasal non-ciliotoxic having particle size 12.32±0.81nm (PdI=0.223) and from kinetic modeling, the release was found to be Fickian diffusion for mucoadhesive microemulsion.

Keywords: Curcumin, intranasal, mucoadhesive microemulsion


How to cite this article:
Patel B M, Mandal S, Rajesh K S. Formulation and kinetic modeling of curcumin loaded intranasal mucoadhesive microemulsion. J Pharm Bioall Sci 2012;4, Suppl S1:81-3

How to cite this URL:
Patel B M, Mandal S, Rajesh K S. Formulation and kinetic modeling of curcumin loaded intranasal mucoadhesive microemulsion. J Pharm Bioall Sci [serial online] 2012 [cited 2020 Jan 26];4, Suppl S1:81-3. Available from: http://www.jpbsonline.org/text.asp?2012/4/5/81/94148

It is a challenge to develop the optimum dosage form of poorly water-soluble chemical entities and simultaneously to target these entities due to their low aqueous solubility followed by limited bioavailability, intra and inter subject variability. [1] To overcome such drawbacks, now various alternative strategies have been explored including nasal route and dosage forms like nanoparticles, emulsions, and solid dispersion etc. Microemulsions (ME) have attracted considerable amount of interest as potential drug delivery systems largely due to their simple method of preparation, stability, solubility enhancement and their abilities to incorporate a wide range of drugs of varying solubility which is expected to enhance the oral. Mucoadhesive microemulsion (MME) increases the residence time by minimizing the nasal drainage so facilitates the absorption process. [2] Curcumin is a water insoluble compound and being a non-invasive method, intranasal administration through microemulsion might be a feasible way of both accommodating relatively higher dose of Curcumin and enhancement of bioavailability.


   Materials and Methods Top


Materials

Curcumin was obtained as a gift sample from Amsar Pvt. Ltd., Goa. Capmul MCM, Accenon, Captex-355 were obtained from Abitec Corporation Ltd., Janeswille, USA. Labrafac, Labrasol, Tanscutol P and Labraphil were obtained from Gattefosse India Pvt. Ltd., Mumbai. Tween-80, Tween-60, Isopropyl myristate, Oleic acid and Soyabean oil were obtained from S.D. Fine Chemicals Ltd., Mumbai. Carbopol 934P was obtained from CDH, New Delhi.

Pseudo-ternary phase diagram

Pseudo-ternary phase diagrams were constructed to obtain the appropriate components and their concentration ranges that result in large existence area of microemulsion as shown in [Figure 1]. Different ME were prepared with suitable oil and different ratios of selected surfactant and cosurfactant (1:1, 2:1, 2.5:1, 3:1 and 3.5:1).
Figure 1: Pseudo-ternary phase diagram of microemulsion (a, 3:1 and b, 3.5:1 ratio of S: CoS)

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Preparation and characterization of microemulsion

Curcumin loaded Microemulsion was prepared by water titration method and was optimized through process and formulation optimization. Predetermined amount of the drug was dissolved in the required quantity of oil. Surfactant and cosurfactant in a fixed ratio were added to it. Finally the above mixture was titrated by distilled water with continuous stirring until a transparent and homogenous microemulsion was produced. Developed Microemulsion was characterized for its transparency, globule size and zeta potential, pH and % assay. Mucoadhesive gel of the microemulsion (MMEI) was prepared by using Carbopol P-934 and the gel was neutralized by dimethylamine.

Nasal ciliotoxicity study

Nasal ciliotoxicity studies were carried out using excised sheep nasal mucosa. Excise nasal mucosa was exposed with equal strength of MME, Saline (negative control) and Analgin (positive control) for 1 hr. The mucocilia was then examined with an optical microscope (Nikon Fx-35A, Japan).

In-vitro drug release studies

In vitro release studies of MME, ME and PDS were performed through sheep nasal mucosa using a modified Franz diffusion cell at 37±2°C. Then size of 2.4 nm of excised nasal mucosa was cut and mounted on the receptor compartment of Franz diffusion cell filled with phosphate buffer pH. 6.8 and at fixed time interval sample were withdrawn and analyzed spectrophotometrically at 420 nm. The release profile as shown in [Figure 2] was fitted into kinetic model to know the release profile as shown in [Table 2].
Figure 2: in-vitro release profile of curcumin

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   Result and Discussion Top


Result of the characterization was given in the [Table 1], [Table 2]. The value of polydispersity index (PI) of both cases were found to be below 1.0 (i.e., 0.223) suggesting that stability persists upon dilution. Aggregations will not take place due to slightly negative charge of the droplets leading to the stability of the formulation.
Table 1: Characterization of the formulation

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Table 2: Kinetic model data

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From the in-vitro release study it was found that mucoadhesive microemulsion (Batch M1) showed more sustained release which is shown in the [Figure 2]. Release data was fitted in to the kinetic models which indicate that the release profile is Fickian.


   Conclusion Top


The studies demonstrated that Labrafil M 1944 CS based microemulsion system stabilized by Acenon CC and Transcutol P and mucoadhesive microemulsion system were optimal for intranasal delivery of Curcumin. However, clinical benefits to the risk ratio of the formulation developed in this investigation will decide its appropriateness in the clinical practice. [3]

 
   References Top

1.Merisko-Liversidge EM, Liversidge GG. Drug nanoparticles: Formulating poorly water-soluble compounds. Toxicol Pathol 2008;36:43-8.  Back to cited text no. 1
    
2.Mandal S, Mandal SS. Design and development of carbamazepine mucoadhesive microemulsion for intranasal delivery: An ex-vivo study. Int J Pharma Sci Rev Res 2010;3:56-60.  Back to cited text no. 2
    
3.Illum L. Nasal drug delivery: Problems, possibilities and solutions. J Control Release 2003;87:187-98.  Back to cited text no. 3
    


    Figures

  [Figure 1], [Figure 2]
 
 
    Tables

  [Table 1], [Table 2]


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