Oral Self Emulsifying Powder (SEP) of Lercanidipine hydrochloride with Neusilin®

Issue 29: JANUARY 2013

Oral Self Emulsifying Powder (SEP) of Lercanidipine hydrochloride with Neusilin®

Ref: Venkata Raman Kallakunta, Suresh Bandari , Raju Jukanti, Prabhakar Reddy Veerareddy
Department of Pharmaceutics and Industrial Pharmacy, St. Peter's Institute of Pharmaceutical Sciences, Warangal-506001, Andhra Pradesh, India

INTRODUCTION
Self-Emulsifying Drug Delivery Systems (SEDDS) improve the oral bioavailability of poorly water soluble drugs. However, the traditional SEDDS as liquid dosage forms has limitations such as low drug loading capacity, drug leakage, low stability, excipient-capsule incompatibility and possibility of irreversible drugs/excipients precipitation. To overcome these complications, the liquid SEDDS are adsorbed on to inert carriers to produce solid SEDDS. Neusilin®'s high specific area, increased surface adsorption, porosity, anticaking flow enhancing properties and its ability to keep the drug stable under amorphous state make it one of the best choice carriers today.
Lercanidipine hydrochloride (LCH: a highly lipophilic calcium channel antagonist used in treatment of hypertension) has the oral bioavailability of approximately 10% and shows erratic absorption from gastrointestinal tract which is attributed to extensive first pass metabolism and low solubility.
The liquid SEDDS of LCH was formulated into solid SEDDS as Self-Emulsifying Powder (SEP) by adsorbing on to Neusilin® as carrier.
High dissolution efficiency value of SEP compared with pure drug indicated the increase in dissolution characteristics of LCH in SEP.

SELF-EMULSIFYING POWDER (SEP) OF LCH

POWDER PROPERTIES OF SEP
The amount of Neusilin® US2 adsorbed to produce free flowing powder was 0.5 g/g of SEDDS formulation. The angle of repose value was 30.14° which indicates good flowability.
The scanning electron micrographs in Figure 1 revealed that LCH as
crystalline powder with irregular shaped crystals. However the self-emulsifying powder showed smooth granular particles.
The z-average diameter and polydispersity index of the solid and liquid SEDDS are presented in Table 1.

Table 1. Mean emulsion droplet size, polydispersity index and dispersion time of liquid SEDDS and solid SEP

Table1

Figure 1. Scanning electron micrographs of A) Pure drug and B) Solid SEP

DISSOLUTION PROFILE
In vitro dissolution studies performed for SEP and LCH powder are shown in Figure 2. The maximum percentage of the drug release was within 15 min from the SEP. In the present investigation drug release profile of SEP showed that the formulation had higher drug release profile than the pure LCH powder, ensuring that the SEP preserved the improvement of in vitro dissolution of liquid SEDDS.
The cumulative % drug release from SEP was found to be 92.18± 2.32% within 60 min and was significantly higher than the pure drug (15.43±3.48%) (p<0.0001).

Figure 2. In vitro dissolution profile of pure drug and SEP (Mean ± SD; n = 3)

CONCLUSIONS

Self-emulsifying powder of LCH with improved dissolution profile was successfully prepared using Neusilin® US2 as an adsorbent carrier.

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