Informatics Publishing Limited

M. V. Nagabhushanam ¹, Ch. V . Prasada Rao ², M. Beena Devi ³, J. Suresh Kumar ⁴

Affiliations
1 DCRM Pharmacy College, Inkollu - 523 167, Prakasam (Dt.,) A.P., IN
2 Department of Biotechnology, Acharya Nagarjuna University, Nagarjuna Nagar - 522510, Guntur, A.P., IN
3 Rahul Institute of Pharmaceutical Sciences & Research , Chirala - 523155, Prakasam Dt., A.P., IN
4 Narasaraopeta Institute of Pharmaceutical Sciences, Kotappakonda Road, Yellamanda Post, Narasaraopet - 522601, Guntur Dt., A.P., IN

Abstract

The poor solubility and wettability of a non steroidal anti inflammatory drug, celecoxib leads to poor dissolution and hence, low bioavailability after oral administration. The objective of the present study was to formulate solid dispersions of celecoxib, with water soluble polymers poly vinyl pyrrolidine (PVP K30), poly ethylene glycol (PEG 6000), hydroxypropyl methylcellulose 5cps (HPMC) and a super disintegrant namely pregelatinised starch (PGS) by common solvent and solvent evaporation methods. Solid Dispersions prepared were evaluated for dissolution rate and dissolution efficiency in comparison to the corresponding pure drug. Solid dispersions of celecoxib showed a marked enhancement in dissolution rate and dissolution efficiency. The increasing order of dissolution rate of solid dispersions of celecoxib with various polymers was HPMC > PVP > PEG. Solid dispersions at 2:2:6 ratio of C: HPMC: PGS, a 53.57 fold increase in the dissolution rate of celecoxib was observed. Solid dispersions were characterized by infrared spectroscopy (IR), differential scanning calorimetry (DSC) and X-ray diffractogram (XRD). Solid dispersions in combined carriers gave much higher rates of dissolution than super disintegrant PGS alone. Super disintegrant PGS alone or in combination with hydrophilic polymers could be used to enhance the dissolution rate of poorly soluble drug celecoxib. Finally, in-vitro dissolution studies showed that celecoxib release was greatly improved by formation of solid dispersion.

Keywords

Celecoxib, Solid Dispersions, Dissolution Rate, Solubility, Superdisintegrant.

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P. Shanmukhi ¹, M. V. Nagabhushanam ¹, K. Ashok ², M. Beena Devi ¹

Affiliations
1 D.C.R.M Pharmacy College, Inkollu - 523 167, Prakasam Dt., Andhra Pradesh, IN
2 QIS College of Pharmacy, Ongole - 523 001, Prakasam Dt., Andhra Pradesh, IN

Abstract

In view of increasing bioavailability and percentage drug release by lymphatic drug delivery, Fosinopril loaded solid lipid nanoparticles were prepared by solvent emulsification and evaporation method. In vitro drug release studies revealed that 80% of the drug was being released from the optimized Fosinopril loaded solid lipid nanoparticles (SLNs) in 24hours. Optimized formulation and process parameters resulted in the production of Fosinopril loaded solid lipid nanoparticles with average particle size of 178.8 nm, zeta potential of -21mV and entrapment efficiency of 91.64% of 10 mg loading. In vitro characterization was carried out to evaluate the stability and release characteristics and kinetics. To analyze the release kinetics of drug from SLNs, drug release data was fitted into zero order, Korsmeyer-Peppas equation. Possible mechanisms for drug release might be anomalous diffusion or non-fickian diffusion. FTIR spectra, DSC thermograms revealed no significant interaction between drug and excipients. TEM photographs exhibited nanosized particles of Fosinopril. The stability studies performed for optimized SLN formulation at 4°C, 25°C, showed no significant change in % entrapment efficiency for one month. So, it was concluded that the optimized SLN formulation offers an efficient mode of delivery to the lipophilic antihypertensive drug, Fosinopril.

Keywords

Fosinopril, Solid Lipid Nanoparticles, Solvent Emulsification and Evaporation, Anti Hypertensive Drug.

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