Swapna, Ponnan (2020) Design and Development of Piperine Nanosuspension and its Investigation on Hepatoprotective and Nephroprotective Activities. Masters thesis, Nandha College of Pharmacy, Erode.
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Abstract
The solubility of drug molecule is an important factor that affects the dissolution rate and bioavailability. Piperine is a most abundant alkaloid in pepper, according to the biopharmaceutical classification it belongs to class II drug. The major problem associated with this drug is its poor bioavailability due to its poor solubility in water and dissolution rate. So in order to improve the solubility the drug can be formulated as a nanosuspension system using polymers like soya lecithin, poloxamer 188, poloxamer 407 and TPGS. The main objective of present work is to formulate nanosuspension of piperine thereby improving the bioavailability. The nanosuspension formulation development has to be preceded by preformulation studies including analytical investigation, choice of the analytical methods and preliminary formulation trials. Selection of excipients, which are compatible with the piperine, and also physiologically safe and biocompatible. Data from the preformulation studies minimizes problems in later stage of piperine development and provides necessary groundwork for the successful formulation attempts thus reducing the cost of development of formulated product. Nanosuspension of piperine was prepared by high-pressure homogenization technique by using 1 % piperine in all formulation along with different stabilizers like Soya lecithin (PNS1 & PNS2), Poloxamer 188 (PNS3 & PNS4), Poloxamer 407 (PNS5 & PNS6) in the ratio of 1 % respectively was used. Co-stabilizer TPGS 1 % was added only in formulation PNS1, PNS3, and PNS5. All the six formulation are subjected to various characterization studies like FT-IR, particle size distribution, saturation solubility studies, in-vitro drug release studies, zeta potential analysis, scanning electron microscopy, powder X-ray diffraction, permeation studies and stability studies. The particle size distribution studies of nanosuspension showed that the particle size of different formulations were in the range of 46.55 to 149.2 nm and polydispersity index in the range of 0.241 to 0.540. The formulation PNS3 shows zeta potential value -29.2 mV and the value indicates that the formulation having good stability. Saturation solubility indicating that nanosuspension showing maximum solubility compared to unprocessed drug. The permeability studies was carried out by using cellulose nitrate membrane revealed that all formulations having better membrane permeation compared to unprocessed drug. In-vitro drug release studies SUMMARY AND CONCLUSION Dept. of Pharmaceutics, NCP Erode 82 shows release rate was in the order of PNS3>PNS5>PNS1>PNS4>PNS6>PNS2. poloxamer 188 with TPGS based piperine formulation PNS3 showed maximum invitro release i.e. 92.36 % in 0.1 N HCl and 92.86 % in phosphate buffer at the end of 12 hours. The surfactant increased the solubility of the drug by action of wetting and dispersion. So the dissolution profile of the complex was found to be improved. In FT-IR study all characteristics peak due to pure piperine was appeared in piperine based nanosuspension formulation spectra which shows no remarkable change in their position after successful method of preparation. The drug content determination appears to be reproducible for preparation of piperine nanosuspension. The piperine formulation (PNS3) TPGS surface modified poloxamer 188 based nanosuspension (PNS3) showed high percentage of drug loading which makes the delivery of the drug clinically feasible and its entrapment efficiency was high when compared to other nano formulations. Piperine nanosuspension PNS3 showed enhanced saturation solubility 118.10 ± 0.91 mg/L in 0.1 N HCl and 152.17 ± 0.81 mg/L in phosphate buffer. Saturation solubility indicating that nanosuspension showing maximum solubility compared to unprocessed drug. The in-vitro permeability study PNS3 shows 90.06 % of the drug was diffused from the lyophilized piperine nanosuspension while from the piperine the diffusion was found to be less. Thus the amount of drug diffused through the nitrocellulose membrane has doubled when it is given in the form of nanosuspension. The X-ray diffraction pattern of formulation PNS3 shows reduction in refraction peaks which indicates decrease in the degree of crystallinity. This indicates crystalline form of the drug converted in to amorphous form. The stability study of optimized formulation indicates that the formulation was quite stable at accelerated condition The physical appearance of piperine nanosuspension did not changed when it was stored at 4 ̊ C for 3 months. SEM analysis of the piperine nanosuspension PNS3 was smaller and spherical and it was found that smooth texture with no polymeric aggregates. Hepato and nephro protective study results indicate the pretreatment with piperine nanosuspension significantly attenuated paracetamol induced liver and gentamycin induced renal damage compared to piperine. Therefore the study provides strong evidence for the use of the piperine nanosuspension as hepato and nephro protective activity against paracetamol induced damage in liver and gentamycin induced renal damage.
| Item Type: | Thesis (Masters) |
|---|---|
| Additional Information: | 261810451 |
| Uncontrolled Keywords: | Piperine Nanosuspension, Investigation, Hepatoprotective, Nephroprotective Activities |
| Subjects: | PHARMACY > Pharmaceutics |
| Depositing User: | Ramakrishnan J |
| Date Deposited: | 22 Apr 2022 09:19 |
| Last Modified: | 22 Apr 2022 09:19 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/19359 |
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