Formulation and Evaluation of Bilayered Gastroretentable Mucoadhesive Patch for Stomach-Specific Drug Delivery

Abstract

The aim of the present work was to develop and evaluate stomach-specific controlled release, gastroretentable mucoadhesive patch of lercanidipine HCl. This drug is essentially soluble in gastric pH range of 1- 4 and have a partition coefficient (log p-value) of 6.1; according to this concept, it has been decided to formulate the gastroretentive bioadhesive patch. The patch system consisted of a drug release rate controlling film, using the combination of Eudragit RSPO and RLPO; mucoadhesive film by using the combination of various hydrophilic polymers. Bilayered patch were made by using the selected batch of two films using the layering method and evaluated for the various parameters like in vitro swelling study, ex vivo mucoadhesive strength. Film was folded into a hard gelatin capsule, evaluated for in vitro drug release in pH 1.2 containing 0.2% (w/v) sodium lauryl sulphate (SLS), and in vivo bioavailability in rabbits. Patches could control the drug release up to 12 h, having mucoadhesion strength in the range of 4.05±0.4 N to 4.52±0.12 N. In vivo bioavailability results indicate that the gastroretentive patch system provides a novel way to retain the drug matrix for the longer period of time in a stomach, enhance drug absorption and thereby offer a promising strategy for gastroretentive mucoadhesive drug delivery for the lercanidipine HCl.

Decades of research in drug targeting using gastroretentive drug delivery systems for antihypertensive therapy

“…Formulation of gastroretentable mucoadhesive patch of lercanidipine HCl has been reported by Pandey et al (2013). The patch consisted of a rate controlling film (Eudragit RSPO and RLPO) and a mucoadhesive film of various hydrophilic polymers.…”

“…Mullen, Stevens and Eccleston (2011) got patented an invention in which an active agent is designed to be released in a prolonged manner at a point of time some time after administration of the active agent. The present invention is particularly suitable for administering an agent that may be released while the subject is sleeping, shortly before waking up and continues to administer Losartan (Chen, 2010), propranolol (Chinta, Graves, Pamujula, 2009;Srikanth et al, 2012), furosemide (Ozdemir, Ordu, Ozkan, 2000;Sahu, Singh, Verma, 2011), verapamil (Elkheshen, Yassin, 2004;Sawicki, 2002), captopril (Martinez, Ramirez, Robles, 2010;Nur, Zhang, 2000), nimodipine (Barmpalexis, Kachrimanis, Georgarakis, 2011;Wu et al, 1997), nicorandil (Nath, Ahmed, 2016), quinapril (Mali, Bathe, 2015), amlodipine (Ramasubramaniyan et al, 2015), atenolol (Charan, Meher, Pochaiah, 2013), metoprolol (Ratnaparkhi, Garje, Chaudhari, 2013) Microspheres Lacidipine (Sultana et al, 2009), diltiazem (Ma et al, 2008), propranolol (Adebisi, Conway, 2011;Patel et al, 2006), furosemide (Iannuccelli et al, 2000), verapamil (Tanwar, Naruka, Ojha, 2008), nifedipine (Soppimath et al, 2006), carvedilol (Zhang et al, 2016) Capsules Nicardipine (Moursy et al, 2003), lisinopril (Semwal's, 2014), lercanidipine (Pandey et al, 2013) Granules Diltiazem (Shimpi et al, 2004) Films Furosemide (Darandale, Vavia, 2012), captopril (Sathish et al, 2013;Pathak, Mishra, 2013) Beads Diltiazem (Saxena et al, 2016), furosemide (ElMeshad, El-Ashmoony, 2012), verapamil …”

Polymer-Based Nanoparticles as Drug Delivery Systems for Purines of Established Importance in Medicine

“…These polymers are also helpful for gastrointestinal (GI) retention, enteric coatings, pulsed release, and transdermal systems. A limited content of methacrylic acid ester with quaternary ammonium groups makes the polymers permeable [2,[17][18][19][20][21][22].…”

pH-triggered drug release from biodegradable microwells for oral drug delivery

“…In this respect, Eudragit ® polymers have been successfully employed in many studies as biocompatible coatings for oral dosage forms. Eudragit ® polymers can be utilized to facilitate a slower drug release, which may lead to an enhancement of drug absorption and a prolonged drug effect (Pandey et al 2013). They may also be used in order to facilitate controlled drug release in selected areas of the GI tract (Luppi et al 2009;Zhu et al 2011).…”

“…upon encountering the higher pH of the small intestine then allows for drug exposure and absorption (Pandey et al 2013). …”