INVESTIGATION OF PRONIOSOMES GEL AS A PROMISING CARRIER FOR TRANSDERMAL DELIVERY OF GLIMEPIRIDE

Objectives: The aim of the study was to develop a proniosomal carrier system that is capable of efficiently delivering entrapped glimepiride over an extended period of time for the treatment of type 2 diabetes. Methods:  Proniosomal gels were developed based on span 60 with and without cholesterol. The entrapment efficiency of drug inside niosomes developed from hydration of the proniosomes gel was also characterized. The in vitro release and skin permeation of glimepiride from various proniosomes gel formulations were investigated. The stability studies were performed at 4°C and at room temperature. Results: The maximum entrapment efficiency was obtained when the cholesterol concentration was 10% of total lipid (90.02%). In vitro release through mixed cellulose ester membrane showed sustained release of drug from proniosomes gels. In vitro drug permeation across rabbit skin revealed improved drug permeation and higher transdermal flux with proniosomes gels compared to hydro-alcoholic gel of drug. Also, good physical stability was also achieved with proniosomes gels. Kinetics of in vitro skin permeation showed diffusion model of drug release from formulations. Conclusion: The study proved that the concentration of cholesterol had great influence on the properties of proniosomes gels. Hence, proniosomes preparation containing 10% cholesterol can significantly increase trans-epidermal flux and prolong the release of glimepiride.         Peer Review History: Article received on- 10 November   Revised on- 14 December       Accepted on- 16 December,  Available online 15 January 2017 Academic Editor: Dr. Asia Selman Abdullah, Al-Razi university, Department of Pharmacy, Yemen, [email protected] 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: 5.5/10 Average Peer review marks at publication stage: 7.5/10 Reviewer(s) detail: Dr. Heba M. Abd El-Azim, Damanhour University, Egypt, [email protected] Dr. Mohamed Derbali, Faculty of Pharmacy, Monastir, Tunisia, [email protected] Similar Articles: PREPARATION AND CHARACTERIZATION OF TOLTERODINE TARTRATE PRONIOSOME

EFFECT OF PEGYLATED EDGE ACTIVATOR ON SPAN 60 BASED- NANOVESICLES: COMPARISON BETWEEN MYRJ 52 AND MYRJ 59

Objective: In recent years, Span 60 based nanovesicles have been the object of growing scientific attention as an alternative potential drug delivery system to conventional liposomes. Surface modification of nanovesicles can adjust the drug release rate and the affinity for the target site. The aim of present work was firstly to study the effects of different PEGylated edge activator (Myrj 52 and Myrj 59) on Span 60 based nanovesicles.Methods: Nanovesicles were prepared using Span 60 alone or in combination with Myrj 52 (polyethylene glycol 2000 monostearate) or Myrj 59 (polyethylene glycol 4400 monostearate) by employing the ethanol injection method. Myrj 52 and Myrj 59 are hydrophilic nonionic surfactants were used to modify the surface of the developed vesicles. Dynamic light scattering was used to determine the size, zeta potential and polydispersity index of the nanovesicles formulation. The vesicles were also characterized for entrapment efficiency and in vitro release.Results: In current work, the modified nanovesicles size (ranging from 54.32 to 141.7 nm), zeta potential (ranging from -5.67 to -27.1 mV) and polydispersity index (ranging from0.248 to 0.531) indicated that the surface modified nanovesicles vesicles are a homogenous and mono-disperse nanovesicles dispersions. The non-modified nanovesicles are showed higher particles size (>2 times) compared to modified nanovesicles. The modified nanovesicles were showed entrapment efficiency ranging from 36.42 to 78.13 %. All the modified nanovesicles showed accepted in vitro release of TN from nanovesicles (>70% released after 8 h), followed Higuchi models as drug release mechanism.Conclusion: In conclusion, these surface modified nanovesicles could be used as a potential drug carrier for a variety of drugs.                     Peer Review History: Received 16 July 2019;   Revised 12 August; Accepted 9 September, Available online 15 September 2019 Academic Editor: Prof. Dr. Gorkem Dulger, Duzce University, Turkey, [email protected] 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: 6.5/10 Average Peer review marks at publication stage: 9.5/10 Reviewer(s) detail: Dr. Robert Tungadi, State University of Gorontalo, Indonesia, [email protected] Prof. Dr. Kapil Kumar, Global Institute of Pharmaceutical Education and Research, Kashipur, US Nagar, Uttarakhand, India, [email protected] Similar Articles: SCREENING STUDY FOR FORMULATION VARIABLES IN PREPARATION AND CHARACTERIZATION OF CANDESARTAN CILEXETIL LOADED NANOSTRUCTURED LIPID CARRIER

Maximization of the in vitro transcorneal release and the in vivo IOP-lowering effects of Latanoprost ophthalmic gel formulations using Azone as a penetration enhancer and Carbopol-974® as a mucoadhesive.

The objective of this study was to maximize the in vitro transcorneal release, the intraocular pressure (IOP) lowering effect and the duration of action, of the Latanoprost acid (LAT) ophthalmic gels. The in vitro transcorneal release of LAT from a first set of gel formulations containing different concentrations of Azone (as enhancer) with a fixed concentration of C-974® (as mucoadhesive) was studied. The formulation that showed the greatest permeability at the lowest Azone concentration was selected for the preparation of a second set of ocular gels containing different C-974® concentrations. Their in vitro permeabilities were evaluated, and the C-974® concentration yielding the greatest in vitro permeability was chosen. The in vivo IOPlowering efficacy study for the scaled-up formulations from both sets of the test formulations was performed using a Tono-pen Avia® tonometer in rabbits for 4 consecutive days. To determine the duration of action, the most effective formulations were used for a single-dose study, and the IOP was measured at predetermined intervals until the IOP base-line was reestablished. The majority of the tested formulations showed significant but varied augmentations in both the in vitro and in vivo permeability results. The formulations GAZ-4 and GC-4 showed the greatest IOP lowering effects, i.e., 7.8±1.8 mmHg and 6.5±2.1 mm Hg, respectively. It is particularly noteworthy that for both formulations the IOP lowering effect continued for 24 hours. Their duration of action in the single-dose study were 47±2.25 hours and 48±1.5 hours, respectively. It was concluded that the in vitro release, onset, magnitude and duration of action of the LAT gels were increased and extended for up to 2 days for the two gel formulations

EFFECT OF PEGYLATED EDGE ACTIVATOR ON SPAN 60 BASED- NANOVESICLES: COMPARISON BETWEEN MYRJ 52 AND MYRJ 59

Objective: In recent years, Span 60 based nanovesicles have been the object of growing scientific attention as an alternative potential drug delivery system to conventional liposomes. Surface modification of nanovesicles can adjust the drug release rate and the affinity for the target site. The aim of present work was firstly to study the effects of different PEGylated edge activator (Myrj 52 and Myrj 59) on Span 60 based nanovesicles.Methods: Nanovesicles were prepared using Span 60 alone or in combination with Myrj 52 (polyethylene glycol 2000 monostearate) or Myrj 59 (polyethylene glycol 4400 monostearate) by employing the ethanol injection method. Myrj 52 and Myrj 59 are hydrophilic nonionic surfactants were used to modify the surface of the developed vesicles. Dynamic light scattering was used to determine the size, zeta potential and polydispersity index of the nanovesicles formulation. The vesicles were also characterized for entrapment efficiency and in vitro release.Results: In current work, the modified nanovesicles size (ranging from 54.32 to 141.7 nm), zeta potential (ranging from -5.67 to -27.1 mV) and polydispersity index (ranging from0.248 to 0.531) indicated that the surface modified nanovesicles vesicles are a homogenous and mono-disperse nanovesicles dispersions. The non-modified nanovesicles are showed higher particles size (>2 times) compared to modified nanovesicles. The modified nanovesicles were showed entrapment efficiency ranging from 36.42 to 78.13 %. All the modified nanovesicles showed accepted in vitro release of TN from nanovesicles (>70% released after 8 h), followed Higuchi models as drug release mechanism.Conclusion: In conclusion, these surface modified nanovesicles could be used as a potential drug carrier for a variety of drugs.                     Peer Review History: Received 16 July 2019;   Revised 12 August; Accepted 9 September, Available online 15 September 2019 Academic Editor: Prof. Dr. Gorkem Dulger, Duzce University, Turkey, [email protected] Received file:                Reviewer's Comments: Average Peer review marks at initial stage: 6.5/10 Average Peer review marks at publication stage: 9.5/10 Reviewer(s) detail: Dr. Robert Tungadi, State University of Gorontalo, Indonesia, [email protected] Prof. Dr. Kapil Kumar, Global Institute of Pharmaceutical Education and Research,Kashipur, US Nagar, Uttarakhand, India, [email protected] Similar Articles: SCREENING STUDY FOR FORMULATION VARIABLES IN PREPARATION AND CHARACTERIZATION OF CANDESARTAN CILEXETIL LOADED NANOSTRUCTURED LIPID CARRIER