Publications by authors named "Fatima Rasool"

14 Publications

  • Page 1 of 1

Simvastatin nanoparticles loaded polymeric film as a potential strategy for diabetic wound healing: in vitro and in vivo evaluation.

Curr Drug Deliv 2021 Jul 20. Epub 2021 Jul 20.

Punjab University College of Pharmacy, University of the Punjab, Lahore, Pakistan.

Introduction: The pleiotropic effects of statins are recently explored for wound healing through angiogenesis and lymph-angiogenesis that could be of great importance in diabetic wounds.

Aim: Aim of the present study is to fabricate nanofilm embedded with simvastatin loaded chitosan nanoparticles (CS-SIM-NPs) has been reported herein to explore the efficacy of SIM in diabetic wound healing.

Methods: The NPs, prepared via ionic gelation, were 173nm ± 2.645 in size with a zeta potential -0.299 ± 0.009 and PDI 0.051 ± 0.088 with excellent encapsulation efficiency (99.97%). The optimized formulation (CS: TPP, 1:1) that exhibited the highest drug release (91.64%) was incorporated into polymeric nanofilm (HPMC, Sodium alginate, PVA), followed by in vitro characterization. The optimized nanofilm was applied to the wound created on the back of diabetes-induced (with alloxan injection 120 mg/kg) albino rats.

Results: The results showed significant (p < 0.05) improvement in the wound healing process compared to the diabetes-induced non-treated group. The results highlighted the importance of nanofilms loaded with SIM-NPs in diabetic wound healing through angiogenesis promotion at the wound site.

Conclusion: Thus, CS-SIM-NPs loaded polymeric nanofilms could be an emerging diabetic wound healing agent in the industry of nanomedicines.
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http://dx.doi.org/10.2174/1567201818666210720150929DOI Listing
July 2021

Fixed Dose Single Tablet Formulation with Differential Release of Amlodipine Besylate and Simvastatin and Its Pharmacokinetic Profile: QbD and Risk Assessment Approach.

Drug Des Devel Ther 2021 24;15:2193-2210. Epub 2021 May 24.

Punjab University College of Pharmacy, University of the Punjab, Lahore, Pakistan.

Purpose: A differential release fixed dose matrix tablet of amlodipine besylate (AML-B) and simvastatin (SIM) was formulated to enhance patient compliance.

Material And Method: In the first phase, release controlling parameters of AML-B and SIM granules were identified and in the second phase a fixed dose AML-B and SIM tablet formulation was prepared and optimized for a differential release of the drugs using a quality by design (QbD) and risk assessment approach. A validated HPLC method was employed for simultaneous determination of AML-B and SIM for FDC formulation. A pharmacokinetics of the above drugs was studied in healthy dogs in the third phase.

Results: In QbD-based optimized formulation, Eudragit RSPO-dicalcium phosphate (DCP) blend controlled the release of AML-B over 8 h, though this diffusion-controlled release assumed first order kinetics. DCP and Eudragit RS 100 also retarded release of SIM causing SIM release over 8 h after AML-B release from the optimized FDC tablet formulation. The HPLC retention times of AML-B and SIM were 2.10 and 15.52 min, respectively. Linearity for AML-B was 5.0-50 ng/mL and 0.01-2.0 µg/mL for SIM with percent recoveries of 92.85-101.53% and 94.51-117.75% for AML-B and SIM. AUC of AML-B was increased 3 fold, while AUC of SIM was decreased 2 fold. The t values for AML-B and SIM were 12 and 6 h, respectively. AML-B was absorbed without any lag time (t) while t was 6.33 ± 0.81 h for SIM, thus met the study objective.

Conclusion: The pharmacokinetic study showed an immediate absorption of AML-B while that of SIM was withheld for 6 h, close to the desired delay time of 8 h.
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http://dx.doi.org/10.2147/DDDT.S240506DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8164448PMC
November 2021

Development and characterization of orodispersible film containing cefixime trihydrate.

Drug Dev Ind Pharm 2020 Dec 6;46(12):2070-2080. Epub 2020 Nov 6.

Faculty of Pharmacy, University of Central Punjab, Lahore, Pakistan.

Patients suffering from dysphagia have trouble in swallowing conventional oral dosage forms and there is also risk of choking, which may cause patient noncompliance. This study aimed to develop an orodispersible film (ODF) containing cefixime trihydrate (CFX) to cope with the above-mentioned problems as well as to enhance water solubility and masking the bitter taste of the drug. The freeze-drying and kneading methods were used for the formation of inclusion complexes. The physicochemical evaluation revealed that T7 was the best film for the incorporation of pure drug and inclusion complexes. Films were further characterized for physical and mechanical properties. Drug content, dissolving time of the film and drug release tests were performed. taste and disintegration time studies were also conducted in healthy human volunteers. FTIR spectra of the individual ingredients and prepared formulations have confirmed the chemical compatibilities of the ingredients. The solubility of CFX was increased by complexation with -CD and optimized freeze-dried inclusion complex (FD1) was selected for the formation of ODF. C4 was selected as an optimized film for the delivery of CFX as this film has released 95.52% drug at the end of 10 min. Dissolution kinetics of FD1 showed that it followed zero-order kinetics while drug release from films, exhibits first-order kinetics; however, both showed non-Fickian transport. taste evaluation revealed that taste was masked by inclusion complexation with β-CD. However, selected ingredients and employed methodology enabled to formulate film, capable of delivering taste-masked CFX with improved solubility and better patient compliance.
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http://dx.doi.org/10.1080/03639045.2020.1843477DOI Listing
December 2020

Artificial Neural Network (ANN) Approach to Predict an Optimized pH-Dependent Mesalamine Matrix Tablet.

Drug Des Devel Ther 2020 22;14:2435-2448. Epub 2020 Jun 22.

Faculty of Pharmacy, Rippha International University, Lahore, Pakistan.

Background: Severe bleeding and perforation of the colon and rectum are complications of ulcerative colitis which can be treated by a targeted drug delivery system.

Purpose: Development of colon-targeted delivery usually involves a complex formulation process and coating steps of pH-sensitive methacrylic acid based Eudragit. The current work was purposefully designed to develop dicalcium phosphate (DCP) facilitated with Eudragit-S100-based pH-dependent, uncoated mesalamine matrix tablets.

Materials And Methods: Mesalamine formulations were compressed using wet granulation technique with varying compositions of dicalcium phosphate (DCP) and Eudragit-S100. The developed formulations were characterized for physicochemical and drug release profiles. Infrared studies were carried out to ensure that there was no interaction between active ingredients and excipients. Artificial neural network (ANN) was used for the optimization of final DCP-Eudragit-S100 complex and the experimental data were employed to train a multi-layer perception (MLP) using quick propagation (QP) training algorithm until a satisfactory root mean square error (RMSE) was reached. The ANN-aided optimized formulation was compared with commercially available Masacol.

Results: Compressed tablets met the desirability criteria in terms of thickness, hardness, weight variation, friability, and content uniformity, ie, 5.34 mm, 7.7 kg/cm 585±5 mg (%), 0.44%, and 103%, respectively. In-vitro dissolution study of commercially available mesalamine and optimized formulation was carried out and the former showed 100% release at 6 h while the latter released only 12.09% after 2 h and 72.96% after 12 h which was fitted to Weibull release model with b value of 1.3, indicating a complex release mechanism.

Conclusion: DCP-Eudragit-S100 blend was found explicative for mesalamine release without coating in gastric and colonic regions. This combination may provide a better control of ulcerative colitis.
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http://dx.doi.org/10.2147/DDDT.S244016DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7320029PMC
March 2021

Expression Profiles and Biochemical Analysis of Chemosensory Protein 3 from Nilaparvata lugens (Hemiptera: Delphacidae).

J Chem Ecol 2020 Apr 3;46(4):363-377. Epub 2020 Mar 3.

Hubei Insect Resources Utilization and Sustainable Pest Management Key Laboratory, College of Plant Science and Technology, Huazhong Agricultural University, Wuhan, 430070, People's Republic of China.

Insects have evolved highly sensitive olfactory sensory systems to detect plant hosts and mates, with plant volatiles playing an important role in informing insect behavior. Chemosensory proteins (CSPs) are thought to play a key role in this process, but in this respect, there is limited information on brown planthopper Nilaparvata lugens, one of the most destructive pests of rice. To expand our understanding of CSP function in N. lugens we explored expression profiles and binding characteristics of NlugCSP3. The ligands with higher binding affinity were also validated by molecular docking and behavioral assays. NlugCSP3 mRNA was expressed at relatively higher levels in antennae and abdomen of 3-day-old unmated macropterous males as well as in antennae of 3-day mated macropterous and brachypterous females. Fluorescence competitive binding assays revealed that 5 out of 25 candidate volatiles are strong binders (Ki < 10 μM). Behavioral assays revealed that nonadecane and 2-tridecanone, which have high binding affinities in fluorescence competition-binding assays, displayed strong attractiveness to N. lugens. Pursuing this further, molecular docking analysis identified key amino acid residues involved in binding volatile compounds. Overall, our data provide a base for further investigation of the potential physiological functions of CSP3 in Nilaparvata lugens, and extend the function of NlugCSP3 in chemoreception of N. lugens.
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http://dx.doi.org/10.1007/s10886-020-01166-6DOI Listing
April 2020

Towards fast and cost-effective up-scaling of Nano-encapsulations by Ionic-gelation method using model drug for the treatment of atopic dermatitis.

Pak J Pharm Sci 2019 Sep;32(5(Supplementary)):2299-2304

Institute of Pharmaceutical Sciences, University of Veterinary and Animal Sciences (UVAS), Lahore, Pakistan.

Chitosan nanoparticles (CSNPs) have proven their excellent drug delivery potential through various routes of administration and therefore, the need for large scale production of CSNPs for the commercialization is paramount. Their particle size and surface charge, drug loading capacity, and morphology were characterized in this study. Finally, drug release studies of both continuous and scalable modes were undertaken to ascertain suitability of CSNPs as a carrier for HC. The particle size of the large and small scale of HC-CSNPs was 253.3±16.4 nm and 225.4 ±9.6 nm, respectively. Besides, the surface charge of the large and small scale of HC-CSNPs was +35.3±0.3 mV and +32.6±2.5 mV, respectively. The size and surface charge of both HC-CSNPs were not proven to be statistically different. Drug loading capacity of large and small scale production of HC-CSNPs was high with 89%, and 83% of HC was loaded into CSNPs, respectively. Moreover, the morphology of both large and small scale production of HC-CSNPs had a similar shape and particle size. The drug release profile of CSNPs prepared by both methods showed a significantly (p<0.05) higher percentage release as compared to the free form. It is expected that positively charged nano-sized HC-CSNPs with high drug loading capacity could enhance the efficiency of drug delivery system to carry and diffuse into the target cells. The results obtained also suggested that the modified method applied could be further developed for large scale production of HC-CSNPs.
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September 2019

Evolution of Deeper Rooting 1-like homoeologs in wheat entails the C-terminus mutations as well as gain and loss of auxin response elements.

PLoS One 2019 4;14(4):e0214145. Epub 2019 Apr 4.

PARC Institute for Advanced Studies in Agriculture, National Institute for Genomics and Advanced Biotechnology (NIGAB), NARC, Islamabad, Pakistan.

Root growth angle (RGA) in response to gravity controlled by auxin is a pertinent target trait for obtainment of higher yield in cereals. But molecular basis of this root architecture trait remain obscure in wheat and barley. We selected four cultivars two each for wheat and barley to unveil the molecular genetic mechanism of Deeper Rooting 1-like gene which controls RGA in rice leading to higher yield under drought imposition. Morphological analyses revealed a deeper and vertically oriented root growth in "NARC 2009" variety of wheat than "Galaxy" and two other barley cultivars "Scarlet" and "ISR42-8". Three new homoeologs designated as TaANDRO1-like, TaBNDRO1-like and TaDNDRO1-like corresponding to A, B and D genomes of wheat could be isolated from "NARC 2009". Due to frameshift and intronization/exonization events the gene structures of these paralogs exhibit variations in size. DRO1-like genes with five distinct domains prevail in diverse plant phyla from mosses to angiosperms but in lower plants their differentiation from LAZY, NGR and TAC1 (root and shoot angle genes) is enigmatic. Instead of IGT as denominator motif of this family, a new C-terminus motif WxxTD in the V-domain is proposed as family specific motif. The EAR-like motif IVLEM at the C-terminus of the TaADRO1-like and TaDDRO1-like that diverged to KLHTLIPNK in TaBDRO1-like and HvDRO1-like is the hallmark of these proteins. Split-YFP and yeast two hybrid assays complemented the interaction of TaDRO1-like with TOPLESS-a repressor of auxin regulated root promoting genes in plants-through IVLEM/KLHTLIPNK motif. Quantitative RT-PCR revealed abundance of DRO1-like RNA in root tips and spikelets while transcript signals were barely detectable in shoot and leaf tissues. Interestingly, wheat exhibited stronger expression of TaBDRO1-like than barley (HvDRO1-like), but TaBDRO1-like was the least expressing among three paralogs. The underlying cause of this expression divergence seems to be the presence of AuxRE motif TGTCTC and core TGTC with a coupling AuxRE-like motif ATTTTCTT proximal to the transcriptional start site in TaBDRO1-like and HvDRO1-like promoters. This is evident from binding of ARF1 to TGTCTC and TGTC motifs of TaBDRO1-like as revealed by yeast one-hybrid assay. Thus, evolution of DRO1-like wheat homoeologs might incorporate the C-terminus mutations as well as gain and loss of AuxREs and other cis-regulatory elements during expression divergence. Since root architecture is an important target trait for wheat crop improvement, therefore DRO1-like genes have potential applications in plant breeding for enhancement of plant productivity by the use of modern genome editing approaches.
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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0214145PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6448822PMC
December 2019

Phytocosmeceutical formulation development, characterization and its in-vivo investigations.

Biomed Pharmacother 2018 Nov 22;107:806-817. Epub 2018 Aug 22.

Department of Pharmacy, Faculty of Pharmacy and Alternative Medicines, The Islamia University of Bahawalpur, 63100, Pakistan. Electronic address:

Several plants found rich in flavonoid, polyphenols, and antioxidants reported antiaging, oppose inflammation and carcinogenic properties but have rarely been applied in dermatology. The present study was an active attempt to formulate a stable phytocosmetic emulsion system loaded with 2% pre-concentrated Prosopis cineraria bark extract, aiming to revive facial skin properties. In order to obtain potent therapeutic activities, we first prepared extracts of stem, leaves, and bark and screen them on basis of phenolic, flavonoids contents and antioxidant, antibacterial, lipoxygenase and tyrosinase inhibition activities. Furthermore, cytocompatibility of the extract was also determined prior starting in vivo investigations. Then the in vivo performance of 2% bark extract loaded emulsion formulation was determined by using non-invasive probe cutometer and elastometer with comparison to base formulation. The preliminary experiment showed that bark extract has a significant amount of phenolic and flavonoid compounds with eminent antioxidant potential. Furthermore, indicated an efficient antibacterial, lipoxygenase, and tyrosinase enzyme inhibition activities. Importantly, the bark extract did not induce any toxicity or apoptosis, when incubated with HaCat cells. Moreover, the in vivo results showed the formulation (size 3 μm) decreased the skin melanin, erythema and sebum contents up to 2.1-,2.7-and 79%, while increased the skin hydration and elasticity up to 2-folds and 22% as compared to the base, respectively. Owing to enhanced therapeutic effects the phytocosmetic formulation proved to be a potential skin whitening, moisturizer, anti-acne, anti-wrinkle, anti-aging therapy and could actively induce skin rejuvenation and resurfacing.
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http://dx.doi.org/10.1016/j.biopha.2018.08.024DOI Listing
November 2018

Eudragit FS based colonic microparticls of metoprolol tartrate.

Acta Pol Pharm 2012 Mar-Apr;69(2):347-53

Faculty of Pharmacy and Alternative Medicines, Islamia University of Bahawalpur, Bahawalpur-63100, Pakistan.

Metoprolol, a cardioselective β-blocker, is well absorbed in colon after oral administration with mean elimination half life of 3 h with bioavailability 50% due to extensive first pass effect, thus it was aimed to develop its modified release dosage form to reduce dosing frequency. Metoprolol tartrate loaded Eudragit FS microparticles were formulated using solvent evaporation technique by varying polymer contents and then compressing into tablets. The dissolution test was performed in simulated gastrointestinal fluid. All tabletted microparticles were tested for stability after storage in accelerated conditions. As a result of various analytical tests like FTIR, XRD and DSC analyses, drug was found stable in the microparticles. Metoprolol tartrate loaded Eudragit FS tabletted microparticles were stable in accelerated storage conditions. The release behavior of pH-dependent formulations was affected by the dissolution medium pH and the concentration of polymer used. There was a decrease in drug release rate with the increase in polymer concentration. In vitro drug release data (except test formulation F3) were best fitted to zero order model, which indicated the controlled release nature of formulation, while the Korsmeyer-Peppas model explored that drug release occurred according to case II relaxation transport mechanism (n > 0.89). Based on the results, it can be concluded that Eudragit FS is a suitable polymer to design pH dependent microparticles using solvent evaporation technique for the release of drug in colon and T2 can be considered as an optimum formulation on the basis of model independent (f2 test) kinetic interpretation of dissolution results (f2 < 50 for T2 versus reference).
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May 2012

A novel granulation non-solvent addition method containing hydrophilic and lipophilic drugs.

Acta Pol Pharm 2012 Mar-Apr;69(2):285-90

Department of Pharmacy, Faculty of Pharmacy & Alternative Medicine, Islamia University of Bahawalpur, Bahawalpur, Pakistan.

Atenolol and simvastatin were granulated in combination by non-solvent addition coacervation method to treat hypertension orally. Dissolution test was performed in water containing 0.5% sodium dodecyl sulfate at 37 0.05 degrees C. FTIR spectrometry, X-ray diffractometry and thermal analysis confirmed the absence of any chemical interaction between polymer and the entrapped drugs. The granules size was about 280-619 μm. Scanning electron microscopy reported irregular morphology of granules. The entrapment efficiency was approximately 90% for atenolol and 70% for simvastatin. A controlled release behavior of both drugs but a burst release phenomenon of simvastatin from the formulations were observed. In conclusion, granules loaded with a hydrophilic and a lipophilic drug were successfully prepared.
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May 2012

Formulation and characterization of a cream containing terminalia chebula extract.

Forsch Komplementmed 2012 2;19(1):20-5. Epub 2012 Feb 2.

Department of Pharmacy, Faculty of Pharmacy and Alternative Medicine, Islamia University of Bahawalpur, Bahawalpur, Pakistan.

Background: This study aimed to formulate a water-in-oil emulsion (formulation) of Terminalia chebula versus its vehicle (base) as control, and investigate its effects on skin melanin, skin erythema, skin moisture content, and transepidermal water loss (TEWL).

Material And Methods: Base containing no active material, and formulation containing 5% concentrated extract of T. chebula, were developed. Different stability parameters were monitored at 8, 25, and 40 °C, as well as 40 °C + 75% relative humidity, for a period of 4 weeks. It was concluded that the creams remained stable at all storage conditions. Both base and formulation were applied to the cheeks of human volunteers for a period of 8 weeks. Different skin parameters were monitored every week to measure any effect produced by these creams.

Results: Changes in TEWL produced by base and formulation were insignificant (p > 0.05) with respect to time while significant (p ≤ 0.05) with respect to base and formulation. The skin moisture content increased after the application of formulation throughout the study period; this effect was insignificant (p > 0.05) with respect to time while significant (p ≤ 0.05) with respect to base and formulation. Both base and formulation showed insignificant (p > 0.05) effects on skin melanin content with respect to time. Skin erythema was reduced by the formulation. Both base and formulation produced statistically insignificant (p > 0.05) effects on skin sebum.

Conclusion: Both creams were aesthetic with respect to sensory evaluation. T. chebula topical cream showed a positive rejuvenating effect on human skin. Hopefully, this study will encourage more attention towards the research and utilization of herbal medicines.
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http://dx.doi.org/10.1159/000335823DOI Listing
October 2012

In vitro-in vivo correlation study on nimesulide loaded hydroxypropylmethylcellulose microparticles.

Yao Xue Xue Bao 2010 Jun;45(6):772-7

Faculty of Pharmacy & Alternative Medicine, Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.

This study involves mathematical simulation model such as in vitro-in vivo correlation (IVIVC) development for various extended release formulations of nimesulide loaded hydroxypropylmethylcellulose (HPMC) microparticles (M1, M2 and M3 containing 1, 2, and 3 g HPMC, respectively and 1 g drug in each) having variable release characteristics. In vitro dissolution data of these formulations were correlated to their relevant in vivo absorption profiles followed by predictability worth analysis of these Level A IVIVC. Nimaran was used as control formulation to validate developed formulations and their respective models. The regression coefficients of IVIVC plots for M1, M2, M3 and Nimaran were 0.834 9, 0.831 2, 0.927 2 and 0.898 1, respectively. The internal prediction error for all formulations was within limits, i.e., < 10%. A good IVIVC was found for controlled release nimesulide loaded HPMC floating M3 microparticles. In other words, this mathematical simulation model is best fit for biowaiver studies which involves study parameters as those adopted for M3 because the value of its IVIVC regression coefficient is the closest to 1 as compared to M1 and M2.
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June 2010

The effect of binders on the bioavailability of ofloxacin tablets in animal model.

Acta Pol Pharm 2010 Mar-Apr;67(2):185-9

Department of Pharmacy, Faculty of Pharmacy and Alternative Medicines, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.

Present study was undertaken to evaluate the effect of binders on the bioavailability of the drug. Two formulations of ofloxacin were manufactured with two different binders, i.e. gelatin and starch, which were analyzed by different in vitro tests such as dissolution test using USP apparatus II (paddle method) by using 0.1 M HCl solution. For in vivo studies, blood samples were collected through the heparinized syringe at zero time (before dosing) and at 0.5, 1.0, 2.0, 4.0, 6.0, 8.0, 10.0, 12.0, 24.0 hours after the dosing of ofloxacin tablets to 24 rabbits and analyzed by high performance liquid chromatography. Mobile phase consisted of distilled water, acetonitrile and triethylamine (700 : 300 : 1.4, v/v/v). The pH of the mobile phase was adjusted at 2.4 with orthophosphoric acid. The maximum plasma concentration attained after the administration of formulation 1 (containing gelatin) was 7.56 +/- 0.835 microg/mL (the mean +/- SEM) and of formulation 2 (containing starch) was 3.4417 +/- 1.16 microg/mL (the mean +/- SEM). There is also statistically significant difference between the volume of distribution and total body clearance of both formulations. Therefore, formulation 1 is more bioavailable than formulation 2. Thus it can be concluded that binder can affect the bioavailability and pharmacokinetics of a drug.
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April 2010

A comparative study of various microencapsulation techniques: effect of polymer viscosity on microcapsule characteristics.

Pak J Pharm Sci 2009 Jul;22(3):291-300

Department of Pharmaceutics, Faculty of Pharmacy and Alternative Medicines, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.

It is a comparative study of salbutamol sulphate-ethylcellulose microcapsules prepared by three different microencapsulation techniques i.e. coacervation thermal change, solvent evaporation and coacervation non-solvent addition by adjusting the ratio of salbutamol sulphate to ethylcellulose. In vitro release profiles of microcapsules were studied using USP XXIV dissolution apparatus-I in 450 ml double distilled water maintained at 37 degrees C at 50 rpm. Scanning electron microscopic results indicated that all microcapsules were aggregated, whitish and irregular in shape with good entrapment efficiency (86.34 to 97.83), production yield (87.91+/-1.34 to 98.33+/-1.37) and flow properties. Initial burst effect was observed in the drug release behavior from all microcapsules. A slight increase in actual drug loading but profound increase in mean diameter of microcapsules was observed with the increase in the viscosity of ethylcellulose. UV and FTIR spectroscopy, x-ray diffractometry and thermal analysis verified the absence of any strong chemical interaction between drugs and polymer. The drug release from all the formulations followed anomalous diffusion mechanism and was best fit to Higuchi's kinetic model. The results suggest coacervation thermal change as an appropriate approach to develop slow-release multi-unit oral dosage form of salbutamol sulphate suggesting at least twice administration in every 24 hours.
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July 2009
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