Preethi GB
@klepharmblr.org
Assistant Professor
KLE College of Pharmacy
EDUCATION
M.Pharm
RESEARCH INTERESTS
Self Emulsifying Drug Delivery System56818921900
Scopus Publications
Scopus Publications
Preethi Gopalapura Bellaiah, Shivakumar Hagalavadi Nanjappa, and Kumar Madalli Ravi
Open Science Publishers LLP
Nevirapine, a non-nucleoside reverse transcriptase inhibitor, exhibits pH-dependent solubility resulting in poor dissolution limiting its absorption. In the present study, an attempt is made to prepare a self-dispersing lipid formulation (SDLF) involving the novel combination of two drug solubility enhancing strategies, i.e., self-emulsifying system (SES) and solid dispersion (SD). Nevirapine-SES (NV-SES) consisting of an ideal ratio of oleic acid (oil), Cremophor RH 40 (surfactant), and Transcutol (co-surfactant) exhibited good emulsifying properties with maximum drug loading. The NV-SES developed was mixed with an equal quantity of nevirapine: gelucire 50/13 solid dispersion [Nevirapine Solid Dispersion (NV-SD)] to get a novel nevirapine SDLF (NV-SDLF). The NV-SDLF was characterized for its zeta potential, polydispersity index, and particle size, and the results obtained were found to be satisfactory. NV-SDLF was adsorbed on carrier neuciline U2 to get solid NV-SDLF, and solid-state characterization using Differential Scanning Calorimetry (DSC) and Powder X-Ray Diffraction (PXRD) indicated the amorphous nature of the drug in NV-SDLF. The in-vitro drug release of the NV-SDLF was found to be 87.2% ± 0.96% in comparison with nevirapine 28.8% ± 1.02%. In-vivo pharmacokinetic performance of solid NV-SDLF and pure drug suspension was carried out in rats, and a significant two-fold increase (p < 0.05) in area under the curve (AUC) of solid NV-SDLF was observed with respect to nevirapine AUC. Thus, the in-vitro and in-vivo results confirmed that the combined strategies of SES and SD in the formulation of solid NV-SDLF were found to enhance the bioavailability of nevirapine, which could be a promising novel drug delivery system in the management of Acquired Immune Deficiency Syndrome (AIDS).
G. B. Preethi, H. N. Shivakumar, M Ravi Kumar, and N Sweta
Innovare Academic Sciences Pvt Ltd
Objective: Lipid-based formulations have gained much attention, particularly on self-emulsifying drug delivery systems (SEDDS), to improve the oral bioavailability of lipophilic drugs. In the present study, an attempt was made to develop and evaluate prototype SEDDS of poorly soluble antiviral BCS class IV drug etravirine.Methods: Various oils, surfactants and co-surfactants were screened for their suitability in the formulation of SEDDS. Based on the screening, gelucire 44/14, as the oil, labrasol as a surfactant and transcutol HP as the co-surfactant were selected. SEDDS with drug etravirine was formulated and evaluated for emulsifying ability, dilution potential and microscopic properties. The emulsion area for each of the combination of oil and surfactant co-surfactant mixture (Smix) was determined by the construction of pseudo-ternary phase diagrams.Results: The optimized formulation with oil (gelucire 44/14) and Smix (labrasol: transcutol HP, 6:1) in a ratio of 2:8 exhibited a rapid emulsification rate and a good polydispersibility index of 0.103±0.012 indicating uniformity of the formed droplets. The size of the droplets was determined by zetasizer and was found to be in 200 nm range. The drug release from the final formulation after 2hr was found to be 41.15%±0.5 compared to 19.3%±3.8 of pure drug indicating enhanced dissolution profile of the drug.Conclusion: In vitro study illustrated enhanced dissolution rate of formulated prototype SEDDS of BCS class IV drug etravirine for oral delivery.
G. B. Preethi, Sayan Banerjee, H. N. Shivakumar, and M Ravi Kumar
Innovare Academic Sciences Pvt Ltd
Objective: The rationale of the current research work was to formulate and evaluate fast-dissolving tablets of doxazosin mesylate with minimum disintegration time and improved dissolution efficiency using solid dispersion method.Methods: Solid dispersions of doxazosin mesylate and polyethylene glycol 8000 in different ratios were prepared using the kneading method. The prepared solid dispersions were subjected to drug interaction and dissolution studies to select the effective solid dispersion for the formulation of fast-dissolving tablets. Fast dissolving tablets containing drug-polyethylene glycol 8000 solid dispersion (1:3) were prepared using various super-disintegrants such as crospovidone, croscarmellose sodium, mixture and coprocessed crospovidone and croscarmellose sodium in concentration range of 2% and 5% by direct compression technique. The prepared formulations (F1–F16) were evaluated for post compression parameters; hardness, thickness, friability, wetting time, disintegration time, and in–vitro drug release.Results: Drug doxazosin mesylate showed enhanced aqueous solubility of 13.3µg/ml in the presence of polyethylene glycol 8000. Differential scanning calorimetery and Fourier transform infrared spectroscopy studies confirmed no interaction between drug and polyethylene glycol 8000and, drug-polyethylene glycol 8000 solid dispersion showed cumulative drug release of 44.48% in 60 min. Formulated FDT of drug-polyethylene glycol 8000 solid dispersion, containing coprocessed mixture of crospovidone and croscarmellose sodium (5%) exhibited disintegration time of 14.5s with percentage cumulative release of 92.46% in 60 min.Conclusion: The work reasonably concludes that for the formulated doxazosin mesylate-fast dissolving tablets, disintegration time was effectively reduced by the presence of coprocessed mixture of crospovidone and croscarmellose sodium and dissolution efficiency was improved by preparation of solid dispersion with polyethylene glycol 8000.
PreethiB Gopalpura, C Jayanthi, and Sonal Dubey
Springer Science and Business Media LLC
Correspondence to Dr. Gopalpura B Preethi, Department of Pharmaceutics, KLES College of Pharmacy, Rajajinagar, II block, Bangalore 560 010, Karnataka, India. E-mail: preethigb_100@yahoo.com BACKGROUND: A diet with a low glycemic index (GI), rich in dietary Þ ber content, is good for the management of postprandial blood glucose levels (PBG), both in normal people as well as in those with type II diabetes mellitus (type 2 DM). AIM: The present study was carried out to evaluate the effect of food products containing Trigonella foenum-graecum seed (fenugreek) on PBG by determining the GI value of foods in healthy volunteers and in those with type 2DM. METHODOLOGY: Three food products (foods A, B, and C), containing known amounts of fenugreek seeds were prepared and evaluated for their acceptance value. After a stipulated time interval food C (which was found to be the most acceptable of the three) and standard food was given to healthy human volunteers and type 2 DM to determine the area under blood glucose increment (AUC) and the GI value of the food. RESULT: In healthy volunteers and diabetic patients, the GI of food C was 60.4 ± 16.4 and 36.83 ± 12.8, respectively; this is signiÞ cantly (P<0.05) lower than the GI of standard food in the two groups, which was 76.6 ± 16.9 and 46.9 ± 15, respectively. In both healthy volunteers and diabetic patients there is a slower and more sustained glucose release from food C compared to standard food and the AUC is less than that of standard food. CONCLUSION: These results conÞ rm that high Þ ber content is capable of lowering the GI value of the food, and this has a beneÞ cial effect on the PBG levels in persons with type 2 DM as well as in healthy people.
Bharathi.P. Salimath, Arshiya Tabassum, E.G. Anupama, Bindumalini, G.B. Preeti, and Paramahans.V. Salimath
Elsevier BV