C. Aparna’s scientific contributions

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Publications (7)


Enhanced Transdermal permeability of Telmisartan by a novel Nanoemulsion gel
  • Article

January 2015

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156 Reads

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24 Citations

International Journal of Pharmacy and Pharmaceutical Sciences

C. Aparna

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K.S. Rao Patnaik

Objective: Telmisartan is an angiotensin II type I receptor blocker antihypertensive agent with 42% oral bioavailability. The aim of the present investigation was to develop a nanoemulsion gel to enhance bioavailability of poorly water soluble Telmisartan. Methods: Different nanoemulsion components (oil, surfactant and co-surfactant) were selected on the basis of solubility and emulsification ability. Pseudotemary phase diagrams were constructed using aqueous titration method. Carbopol 934 was added as a gel matrix to convert nanoemulsion into nanoemulsion gel. Drug loaded nanoemulsions and nanoemulsion gels were characterized for particle size, viscosity, rheological behavior, thermodynamic stability studies and ex vivo permeation studies using rat skin. Transdermal permeation of Telmisartan from nanoemulsion gels was determined using Franz Diffusion cell. Results: The optimized nanoemulsion gel (NEG) contained Labrafil®M 2125 CS (14.3%) as oil, Acrysol®EL 135 (30.84%) as surfactant, Carbitol® (15.42%) as co-surfactant and (32.44%) water; 20 mg drug and 1% w/w carbopol. The ex vivo permeation profile of optimized formulation was compared to nanoemulsion and normal gel. Permeability parameters like steady-state flux (Jss), permeability coefficient (Kp), and enhancement ratio (Er) were significantly increased in nanoemulsion (NE) and nanoemulsion gel (NEG) as compared to conventional gel. There was a considerable improvement in bio availability for nanoemulsion gel compared to the conventional telemisartan gel. Conclusion: Nanoemulsion gel has significantly increased the bio-availability of the drug. © 2015, International Journal of Pharmacy and Pharmaceutical Science. All rights reserved.


Formulation and evaluation of montelukast sodium and levocetirizine dihydrochloride sublingual tablets

January 2015

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1,667 Reads

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9 Citations

Asian Journal of Pharmaceutical and Clinical Research

Objective: The objective of the current study was to develop and optimize sublingual tablets of montelukast sodium and levocetirizine dihydrochloride which are effective drugs in the treatment of asthma. Methods: The sublingual tablets of montelukast sodium and levocetirizine dihydrochloride were prepared by direct compression method using sodium starch glycolate, crospovidone (CP), and croscarmellose sodium (CCS) as superdisintegrants. The tablets were evaluated for physical properties including hardness, weight variation, thickness, friability, drug content, wetting time, water absorption ratio, in vitro disintegration time, and in vitro dissolution study. Results: The hardness, weight variation, thickness, friability, and drug content of tablets were within pharmacopoeial limits. An optimized tablet formulation F8 was found to have short wetting time of 18.36 seconds, water absorption ratio of 94.42 and in-vitro disintegration time of 45.42 seconds. The results indicated that the amount of super disintegrants such as CP and CCS significantly affected the dependent variables like wetting time, water absorption ratio and in-vitro disintegration time. The in-vitro drug release was found to be higher for formulation F8 with 94.59% for montelukast sodium and 95.48% for levocetirizine dihydrochloride within 60 minutes. The drug release improved by 1.88 times for montelukast sodium and 1.82 times for levocetirizine dihydrochloride compared to oral marketed immediate release tablet formulation. Conclusion: From the present study, it can be concluded that sublingual route has potential to improve the bioavailability of the drug by avoiding first pass metabolism, to provide quicker onset of action and to improve patient compliance in the management of asthma. © 2015, Asian Journal of Pharmaceutical and Clinical Research. All rights reserved.


Formulation and evaluation of oral self emulsifying drug delivery system of lornoxicam

January 2015

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62 Reads

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9 Citations

International Journal of Pharma and Bio Sciences

The objective of the present study is to formulate Self emulsifying drug delivery system (SEDDS) of lornoxicam, an anti-inflammatory drug to sustain the drug release and to reduce the side effects. The study involves combining oils with food grade non ionic emulsifiers to form concentrates that can incorporate large quantities of water and remain as a single phase liquid. Solubility studies were performed to select oils, surfactants and co-surfactants for the formulation. of the drug (BCS class II). In this study, self emulsifying formulations (Batch F1 to F20) of drug Lornoxicam were made using different concentration of Capryol 90, Tween 20, Tween 80, Transcutol P, Propylene glycol. Systematic optimization was carried out, with a goal to minimize self emulsification time, to sustain the percentage drug release and reduce the side effects. The best emulsification grade was with batch F9. The in vitro drug release of Lornoxicam SEDDS was sustained (87.12% for 24 hours) when compared to marketed formulation Lornoxi (tablet) (100% at 90 mins). Pharmaco dynamic studies performed by paw volume method indicated significant (p< 0.05) inhibition in paw edema (75%) for the test formulation after 4 hours as compared to the standard formulation (56%).



Formulation, evaluation and characterization of Glipizide nanoemulsion

June 2013

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452 Reads

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54 Citations

Asian Journal of Pharmaceutical and Clinical Research

The aim of the present study was to formulate, evaluate and characterize the nanoemulsion formulation of Glipizide. Glipizide is a second generation sulphonyl urea drug used in the treatment of noninsulin dependent diabetes mellitus. It has less solubility in water and the half life of the drug is 2-4hrs.Hence by formulating Glipizide nanoemulsion the drug release will be sustained thus dosing intervals will be decreased and it eliminates the variations in the absorption. Solubility studies were conducted to select the oil, surfactant and cosurfactant. Phase diagrams were constructed by aqueous phase titration method. Formulations were selected from the phase diagrams. The prepared nanoemulsions were subjected to different thermodynamic stability tests. The results showed that all the formulations had a good stability. Based on the in vitro drug release studies the formulations were optimized. The optimized formulations were successful in sustaining the drug release for 12hrs. The optimized formulationF9 containing Capryol90 31.5%, Tween 20 15.76%, Transcutol P 32.46% and water 21.0%) optimized formulation F29containing Capryol 90 30.57%, Tween 80 11.83%, Transcutol P 35.51% and water 22.10% showed more than 85% 0f drug release in 12 hrs. The formulations were evaluated for viscosity, pH, percentage transmittance and phase separation. The formulations were also characterized for zeta potential, particle size. The droplet size of the optimized formulation (F9) was found to be 41.6nm and zeta potential was found to be -24.4mV.). Pharmacodynamic studies showed that the optimized formulation (F9) reduced blood glucose levels up to 12 hrs.


Enhancement of dissolution of irbesartan using liquisolid technology

January 2012

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57 Reads

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8 Citations

International Journal of Pharmacy and Technology

Irbesartan is a non peptide, specific competitive antagonist of the angiotensin II receptor antagonist, used orally for the treatment of hypertension. The drug exhibits low bioavailability owing to its poor water solubility. According to BCS, Irbesartan is class II compound i.e. water insoluble and lipophilic, highly permeable drug. Therefore IRB bioavailability can be improved by increasing its solubility and dissolution rate 1. In order to improve solubility by way of dissolution enhancement, we have formulated a liquisolid system of IRB. This method involves dissolving water insoluble drugs in nonvolatile vehicles, which are then converted into free flowing and compressible powders by blending with suitable excipients. Several liquisolid formulations were prepared based on an mathematical model which was used to calculate the required quantities of powder and liquid ingredients, to produce acceptably flowing and compressible admixture. The prepared LS systems were evaluated for the flow properties such as Bulk density, tapped density, Carr's index, Hausner's ratio and angle of repose. Both DSC and XRD results suggested loss of crystallinity of irbesartan upon convertion into a liquisolid formulation. The results showed that liquisolid systems demonstrated considerably higher dissolution rates than plain drug and DCT. This might be due to increased wetting properties and surface of drug available for dissolution.


Immediate and mucoadhesive sustained release compacts of itraconazole using liquisolid technology

14 Reads

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2 Citations

Liquisolid technique was used as a novel approach to develop immediate release and sustained release formulations. Itraconazole was selected as a model drug for this approach. The objective of the study was to increase the dissolution of Itraconazole by formulating it into immediate release compacts and to increase the bioavailability of itraconazole by formulating it into mucoadhesive sustain release compacts. Propylene glycol, PEG 400, PEG 600, Tween 80 and span 80 were used as nonvolatile liquid vehicles. In immediate release formulations Avicel pH 200, Aerosil 200 sodium starch glycolate were used. HPMC K4M, Carbopol 940 and Chitosan were selected as carrier polymer and Aerosil 200 was selected as coating material for mucoadhesive sustained release compacts. It was observed that the percentage drug release for immediate release compact S-8 (optimized) was found to be 100% within 45 mins, whereas marketed capsule (SPORONOX) reported 100% drug release after 90 mins. The mucoadhesive sustained release liquisolid compact MHP-4(HPMC K4M as polymer/carrier) reported sustained activity for 8 h following zero order kinetics with greater mucoadhesion property. © 2015, International Journal of Pharmacy and Technology. All rights Reserved.

Citations (7)


... Spireas (2) proposed liquisolid technology as an approach for both immediate and sustained release formulations. He showed that this simple technique may enable zero order release kinetic in the case of sustained release liquisolid formulations with poorly water-soluble drugs, which was also confirmed in some later studies (31)(32)(33). Sustained drug release from liquisolid formulations can be achieved by using hydrophobic carriers (e.g., Eudragit ® RL and Eudragit ® RS) or by adding a binding (i.e., matrix forming) agent such as hypromellose (2,31,32). ...

Reference:

An Investigation into the Influence of Process Parameters and Formulation Variables on Compaction Properties of Liquisolid Systems
Immediate and mucoadhesive sustained release compacts of itraconazole using liquisolid technology
  • Citing Article

... Many hydrophilic excipients like PEG 4000, PEG 6000, Mannitol, PVP, and poloxamers can be used to enhance the dissolution of drug 7 . Several strategies have been employed to improve the solubility of irbesartan& increase in dissolution rate in aqueous media ( including solid dispersion with various superdisintegrate such as sodium starch glycolate (SSG), crosspovidone (CP), croscarmellose sodium (CCS) and microcrystalline cellulose (MCC) 8 and solid dispersion of irbesartan (IBS), prepared with small molecules such as tartaric acid and mannitol and polymeric additives like polyvinylpyrrolidone (PVP) and hydroxypropyl methylcellulose (HPMC) 9 ), the Liquisolid technology 10 , Particle size reduction by micronization or nanonization 11 , Alteration of the solid state at the particle or molecular level 12 . ...

Enhancement of dissolution of irbesartan using liquisolid technology
  • Citing Article
  • January 2012

International Journal of Pharmacy and Technology

... The percent of light transmittance was determined by a UV-Visible spectrophotometer to preserve double distilled water as blank at 600 nm. Results were being taken in triplicate (20) . ...

Formulation, evaluation and characterization of Glipizide nanoemulsion
  • Citing Article
  • June 2013

Asian Journal of Pharmaceutical and Clinical Research

... In addition, the absorption of the drug by the veins located in the mouth floor, leading directly to the superior vena cava [6] combined with a small thickness of 100-200 µm. Allows faster distribution of the drug through the bloodstream compared to that of orally administered drugs [6][7][8][9][10]. Freeze-dried sublingual tablets have attracted much attention from researchers as it offers tablets of high porosity which allows better exposure of the drug to the saliva in the mouth resulting in immediate disintegration and dissolution of the tablet when placed under the tongue [11][12][13][14][15][16]. ...

Formulation and evaluation of montelukast sodium and levocetirizine dihydrochloride sublingual tablets
  • Citing Article
  • January 2015

Asian Journal of Pharmaceutical and Clinical Research

... Last, the drug's penetration rate from the nanoemulsion may be increased because it is easy to change a drug's affinity for the internal phase to favour partition into the skin. These unique benefits make nanoemulsions a highly effective choice for transdermal drug delivery [24]. ...

Enhanced Transdermal permeability of Telmisartan by a novel Nanoemulsion gel
  • Citing Article
  • January 2015

International Journal of Pharmacy and Pharmaceutical Sciences

... The refractive index of emulsion is compared with water (R.I = 1.333) by putting a drop on the slide of the refractometer. If the refractive index of formulation is same as water having 99% transparency, then that means the formulation is transparent in nature [47]. In-vitro dissolution studies are carried out to note down the drug release per unit time. ...

Formulation and evaluation of oral self emulsifying drug delivery system of lornoxicam
  • Citing Article
  • January 2015

International Journal of Pharma and Bio Sciences