Solid lipid nanoparticles of diethylcarbamazine citrate for enhanced delivery to the lymphatics: in vitro and in vivo evaluation.
OBJECTIVE
The major objective is to target diethylcarbamazine citrate (DEC) to the lymphatics and to increase its retention time. The effect of various excipients on the physicochemical characteristics of the nanoparticles was also studied.


METHODS
Solid lipid nanoparticles (SLNs) of DEC were prepared by ultrasonication by varying the concentrations of compritol 888 ATO, poloxamer 188 and soya lecithin. The SLNs were evaluated for size, shape, texture, surface charge, physical nature of the entrapped drug, entrapment efficiency and in vitro drug release. In vivo animal studies were carried out to estimate the pharmacokinetic parameters in blood and drug concentration in lymph after oral administration.


RESULTS
The size of the spherical particles was in the range of 27.25 ± 3.43 nm to 179 ± 3.08 nm and a maximum entrapment efficiency of 68.63 ± 1.53% was observed. In vitro release studies in pH 7.4 PBS displayed a rapid release and the maximum time taken for the complete drug to release was 150 min. In vivo studies indicated an enhancement in the amount of drug that reached lymphatics when administered via SLNs.


CONCLUSIONS
Targeting of DEC to the lymphatics is possible through SLNs and the retention time in the lymphatics can also be enhanced.
PSG College of Pharmacy, Department of Pharmaceutics , Peelamedu, Coimbatore - 641004, Tamil Nadu , India.
Karthik
K
Siram
Vijaya Raghavan
VR
Chellan
Tamilselvan
T
Natarajan
Balakumar
B
Krishnamoorthy
Habibur Rahman
HR
Mohamed Ebrahim
Vamshikrishna
V
Karanam
Siva Selva Kumar
SS
Muthuswamy
Hari Prasad
HP
Ranganathan
D000284:Administration, Oral; D000818:Animals; D004049:Diethylcarbamazine / Q000008:administration & dosage* / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry*; D005227:Fatty Acids / Q000737:chemistry; D054709:Lecithins / Q000737:chemistry; D008055:Lipids / Q000737:chemistry; D008208:Lymphatic System / Q000378:metabolism; D008297:Male; D053758:Nanoparticles; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013025:Glycine max / Q000737:chemistry; D013997:Time Factors
D004337:Drug Carriers; D005079:Excipients; D005227:Fatty Acids; D054709:Lecithins; D008055:Lipids; D020442:Poloxamer; C086409:glyceryl behenate; D004049:Diethylcarbamazine
diethylcarbamazine citrate; filariasis; lymphatic targeting; mesenteric lymphatic duct; poloxamer 188; solid lipid nanoparticles