Abstract
Objective: Ritonavir is human immunodeficiency virus (HIV) protease inhibitor used as the antiretroviral agent. The objective of the present investigation was to formulate and evaluate Ritonavir gastro-retentive floating microballoons for controlled release. Methods: Five batches of microballoons were prepared by the emulsion solvent diffusion method. The resultant microballoons were evaluated for percentage yield, entrapment efficiency, particle size, and in vitro drug release, stability study. Results: The densities of floating microspheres were found to be less than the density of gastric fluid (1.004 g/cm3). The entrapment efficiency of prepared floating microspheres was satisfactory (68.37 to 88.52%). Among all formulations, FM1 prepared with polymer HPMC was found to be the best as it exhibited highest drug release (89.07%) in 12 hrs and was stable for three months at ambient conditions. Conclusion: Study concludes that Ritonavir can be delivered in the form of floating hollow microballoons in an efficient way. Based on different evaluation parameters, formulations of batch FM1 were found to an optimum formulation. Peer Review History: Received 5 April 2017; Revised 9 May; Accepted 12 May, Available online 15 May 2017 Academic Editor: Ahmad Najib, Universitas Muslim Indonesia, Indonesia, ahmad.najib@umi.ac.id UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file: Reviewer's Comments: Average Peer review marks at initial stage: 3.5/10 Average Peer review marks at publication stage: 7.5/10 Reviewer(s) detail: Dr. Maha Khalifa Ahmed Khalifa, Al-Azhar Universit - Cairo, Egypt, mahakhalifa.ahmed@hotmail.com Prof. Dr. Amani S. Awaad, Prince Sattam Bin Abdulaziz University, Al-Kharj. KSA., amaniawaad@hotmail.com Similar Articles: FORMULATION AND EVALUATION OF ETORICOXIB MICROBEADS FOR SUSTAINED DRUG DELIVERY FORMULATION AND IN-VITRO EVALUATION OF FLOATING MICROBALLOONS OF STAVUDINE FORMULATION AND EVALUATION OF IBUPROFEN GASTRO-RETENTIVE FLOATING TABLETS
Highlights
MATERIALS AND METHODS Ritonavir was obtained from Silva Hill Pharma Limited, Nigeria city, Eudragit L 100 and hydroxypropyl methylcellulose (HPMC) were purchased from the Jagal Pharmaceutical, Lagos, Nigeria
After observing the initial volume of floating microballoons, the tapping was continued on a hard surface until no further change in volume was noted and the tapped density was calculated according to following formula9: 2. Angle of repose The angle of repose of Ritonavir hollow microballoons was determined by fixed funnel method
In vitro release studies A 12 hrs study of drug release rates from floating Ritonavir microballoons was carried out using USP type II dissolution paddle assembly
Summary
The oral route is being used for the delivery of therapeutic agents because of different advantages including the low cost of the therapy and ease of administration lead to high levels of patient compliance. Drugs that are absorbed from the gastrointestinal tract and have a short half-life are eliminated quickly from the blood circulation, so there is a need of frequent dosing to maintain therapeutic concentration of drug. To eliminate this limitation, the oral sustained controlled release formulations have been developed in an attempt to release the drug slowly into the gastro-intestinal tract and maintain an effective drug concentration in the blood over long period of time[3]. Conventional oral dosage forms do not offer any control over drug delivery and cause great fluctuations in plasma drug concentrations[4]. Ritonavir is selected as the model drug to prepare floating micro balloons
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