Development and Characterization of Non-Ionic Surfactant Vesicles (Niosomes) for Oral delivery of Lornoxicam

Niosomes are non-ionic surfactant vesicles obtained on hydration of synthetic nonionic surfactants, with or without incorporation of cholesterol or other lipids. They are vesicular systems similar to liposomes that can be used as carriers of amphiphilic and lipophilic drugs. Niosomes are promising vehicle for drug delivery and being non-ionic, it is less toxic and improves the therapeutic index of drug by restricting its action to target cells. They are lamellar structures that are microscopic in size. They are now widely used as alternative to liposomes. Niosomal dispersion in an aqueous phase can be emulsified in a non-aqueous phase to regulate the delivery rate of drug and administer normal vesicle in external non-aqueous phase. Stable niosome dispersion must exhibit a constant particle size and a constant level of entrapped drug. Span 60 is the better surfactant of all because it is having high phase transition temperature and low HLB (Hydrophilic Lipophilic Balance) so it will form vesicles of good size.one more reason for the selection of span 60 and that was the critical packing factor which is between 0.5 and 1 for this surfactant so it forms spherical vesicles. If CPP factor is below 0.5 it cause micelles to form and if it was above 1 it will form inverted vesicles. Lornoxicam loaded niosomes were prepared by Lipid film hydration method with different surfactant to cholesterol ratio. The niosome formulations were evaluated for FT-IR study,microscopy. The niosomal suspensions were further evaluated for entrapment efficiency, In vitro release study, Kinetic data analysis, Stability study. The formulation F4 which showed higher entrapment efficiency of 80.54 ±0.99. Release was best explained by the zero order kinetics. Kinetic analysis shows that the drug release follows super case II transport diffusion. Niosome formulation has showed appropriate stability for 90 days. *Corresponding author, Mailing address: D. Akhilesh Department of Pharmaceutics, Shree Devi College of Pharmacy, Airport Road, Mangalore (Karnataka). India *E-mail: [email protected] Article History:-----------------------Date of Submission: 27-05-2012 Date of Acceptance: 01-06-2012 Conflict of Interest: NIL Source of Support: NONE F U L L L e n g t h R e s e a r c h P a p e r C o v e r e d i n I n d e x C o p e r n i c u s w i t h I C V a l u e 4 .6 8 f o r 2 0 1 0 Int. J. Drug Dev. & Res., July-September 2012, 4 (3): 147-154 Covered in Scopus & Embase, Elsevier 147 short biological half life (about 3-5 hours) and dosing frequency not more than once a day makes lornoxicam an ideal candidate for sustained release 2. Nowadays considerable interest has been focused on niosomes based targeted drug delivery. Niosomes are non-ionic surfactant vesicles obtained on hydration of synthetic nonionic surfactants, with or without incorporation of cholesterol or other lipids. They are vesicular systems similar to liposomes that can be used as carriers of amphiphilic and lipophilic drugs. Niosomes are promising vehicle for drug delivery and being non-ionic; it is less toxic and improves the therapeutic index of drug by restricting its action to target cells. This systemic review article deals with preparation methods, characterizations, factors affecting release kinetic, advantages, and applications of niosomes.3 Niosomal drug delivery has been studied using various methods of administration including intramuscular intravenous, peroral and transdermal. In addition, as drug delivery vesicles, niosomes have been shown to enhance absorption of some drugs across cell membranes, to localize in targeted organs and tissues and to elude the reticulo endothelial system 4. MATERIALS AND METHODS Lornoxicam obtained as a gift sample from Aeon biologicals Chennai(India). Cholesterol obtained from Merck Specialties Pvt. Ltd., Mumbai (India).Span 60 obtained from national chemicals, Gujrat (India). Chloroform from Suvinadh chemicals, Baroda. Rotary flash evaporator for the preparation of niosomes procured from Popular India, Dialysis membrane for the study of in-vitro release obtained from Hi media India. All other materials used and received were of analytical grade. RESULT AND DISCUSSION Preformulation study FT-IR spectra of lornoxicam were recorded.Main peaks was there at 3068.19 for C=C stretching, 1733 for C C, 1592.9 for the primary and secondary amines and amides(-NH group), 1327.5,1187.9, 1084,1041 for the amines(-C-N group), 831,790 for the aromatic group, 765, 737,689.47,630 for the C-X group, 1041.37 for S=O stretching.So the drug was found to be pure compared to pure drug which is shown in the table below. FTIR spectra of lornoxicam Table 24: Peak no. and position of lornoxicam compared with pure drug Peak no: Position Pure lornoxicam Groups present Range of group s 1 3068.19 3067.06 C=C stretchin g 3100300 3 1592.91 1580.39 -NH 16401550 4,5,6,7 1327.5,1187,108 4, 1323.36,1185.64,1092.9 3 -C-N 13501000 9,10 831 828.83 Aromatic 900690 11,12,1 3 765,737,689.47 764.87,726.7,688.7 -C-X 785540 7 1041.37 1055.33 S=O 10301060 Solubility study 10 mg of lornoxicam is freely soluble in 0.1N NaOH after heating. Preparation of niosomes of lornoxicam The niosome formulations were prepared by lipid film hydration technique. Drug (lornoxicam) is freely soluble in 0.1N NaOH after heating. non ionic surfactant and cholesterol were weighed (surfactant:cholesterol in μmol) and dissolved in chloroform methanol (2:1) in a 100 ml round bottom F U L L L e n g t h R e s e a r c h P a p e r C o v e r e d i n I n d e x C o p e r n i c u s w i t h I C V a l u e 4 .6 8 f o r 2 0 1 0 D. Akhilesh et al: Development and Characterization of Non-Ionic Surfactant Vesicles (Niosomes) for Oral delivery of Lornoxicam Int. J. Drug Dev. & Res., July-September 2012, 4 (3): 147-154 Covered in Scopus & Embase, Elsevier 148 flask. A thin lipid film was formed under reduced pressure in a rotary flash evaporator, temperature was maintained at 600c or above. The film was then hydrated by 10 ml of PBS* pH 7.4 at a temperature above the glass transition temperature of the surfactant with gentle shaking. The niosome suspension obtained was sonicated for 5 min which forms small sized vesicles. The stabilized MLVs were used for further studies. Table 1: Compositions of Niosomal batches of Lornoxicam Formulation No. Ratio (μmol)(surfactant: cholesteol) Surfactant (mg) Cholesterol (mg)