Akila RM

ABSTRACTThe present work is focused on the development, evaluation and statistical optimization of almotriptan malate transdermal patches. Almotriptan malate is used as anti-migraine drug and reported to have the best-sustained pain free rate and the lowest adverse events rate of all the triptans and thus making interest in the development of new route for the therapeutic administration of the drug, So, the present research work was aimed to develop  matrix type transdermal patches  using polymers HPMC K15M, ERS100 and EC and plasticizers DBP and PEG400 by solvent casting method. This formulation would help to avoid non-compliance of the tablet dosage form The IR spectra of the drug and physical mixtures of drug-polymer confirmed the absence of incompatibility between drug and polymers. The in-vitro drug release studies revealed that patches made of HPMC K15M-ERS 100 with DBP as plasticizer was considered as the best formulation and incorporated in 22 factorial design and evaluated for further studies.  The concentration of HPMC K 15M and ERS 100 are chosen as the independent variables.  Drug content, %moisture absorption  %, moisture loss, and cumulative % drug released at 12h are chosen as dependent variables. The drug release from transdermal patches followed zero order kinetics. Various physicochemical parameters of the patches were investigated. The current research work of transdermal patches of almotriptan malate may provide sustained delivery for prolonged periods in the management of migraine, which can be a good way to bypass the extensive hepatic first-pass metabolism. Keywords:  migraine, almotriptan malate, transdermal patches, solvent casting, 22 factorial design

ABSTRACTNanoparticles are designed to improve the pharmacological and therapeutic properties of conventional drugs. In the present research work, almotriptan malate was formulated as nanoparticle drug delivery system for the effective management of migraine by ion-gelation technique. Shape and size of the nanoparticles were evaluated by TEM images. FTIR and  DSC studies confirmed that there were no interactions between the drug and the other ingredients. XRD study was carried out to confirm the crystalline or amorphous nature of the nanoparticles. The entrapment efficiency of was found to be 74 to 82% and drug loading capacity was found to be 15 to 16% The in-vitro release studies concluded that the release was sustained after an initial burst. The in vitro mucoadhesion study using goat nasal mucosa was found to be 54% and 69%. The kinetic study revealed that the almotriptan malate nanoparticles followed the first order kinetics. Keywords: biodegradable chitosan, nanoparticles, almotriptan malate,  mucoadhesion  

Chitosan (N-acetyl D- glucosamine) is a natural polysaccharide present in crustacean shells, some fungi and yeast. It is a versatile polysaccharide irrespective of its sources. In the present research work, fungal chitosan is characterized for its anti proliferative effect on HeLa and MCF-7 tumour cell lines by MTT assay. The results showed that GI50 of fungal chitosan was found to be 75µg/ml and 80µg/ml on HeLa and MCF-7 cells respectively.

In general, as a subclass of epilepsy, nocturnal epilepsy intensify one of the major problems of epilepsy as it is less likely witnessed than daytime epilepsy and therefore it is very difficult to diagnose and characterize and this results in sleep disruption which can cause daytime somnolence and concentration difficulty. So, the present research work was aimed to formulate a programmable pulsatile press coated tablets of levetiracetam inorder to achieve chronotherapy for nocturnal epilepsy. The core tablets containing levetiracetam were prepared by direct compression method and press coated with HPMC K100M and MCC. The prepared pulsatile tablets were evaluated for in-vitro release to get desirable pulsatile release of drug after a lag time of 2.5 h. Drug-excipients compatibility study by IR spectrophotometer showed that all the excipients were compatible with the drug. The stability study was carried out for the desired optimized formulation for a period of 3months and showed insignificant difference.