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Formulation of Gastric Floating System Using Bio-Sourced Terminalia Catappa Gum and in vivo Evaluation

Meka VS, Murthy Kolapalli VR

Curr Drug Deliv, 2016;13(6):971-81.
PMID: 26452534

A central composite design was applied to design a novel gastric floating drug delivery system comprising propranolol HCl in Terminalia catappa gum and to evaluate the buoyancy, in vitro drug release behavior, and pharmacokinetic parameters. All formulations exhibited good buoyancy properties in vitro reflected by floating lag time of 1-110 sec, total floating time of 9-16 h and prolonged release behaviour (upto 12 h). Statistically optimised formulation (PBGRso) was orally administered to human volunteers under both fasted and fed conditions to evaluate gastric floating behavior under different food conditions by X-ray evaluation. In vivo studies of optimised formulations revealed that the gastric residence time of floating tablets was enhanced in the fed but not in the fasted state. Pharmacokinetic studies of the optimised Terminalia catappa formulation and a commercial product (Ciplar LA 80) carried out on healthy human volunteers showed a significant improvement in the bioavailability (132%) of propranolol HCl released from from the experimental Terminalia catappa formulations compared with Ciplar LA 80.
Design and evaluation of a gastroretentive drug delivery system for metformin HCl using synthetic and semi-synthetic polymers

Meka VS, Gorajana A, Dharmanlingam SR, Kolapalli VR

Invest Clin, 2013 Dec;54(4):347-59.
PMID: 24502177

The aim of the present research was to prepare and evaluate a gastroretentive drug delivery system for metformin HCl, using synthetic and semi-synthetic polymers. The floating approach was applied for preparing gastroretentive tablets (GRT) and these tablets were manufactured by the direct compression method. The drug delivery system comprises of synthetic and semi-synthetic polymers such as polyethylene oxide and Carboxymethyl ethyl cellulose (CMEC) as release-retarding polymers. GRT were evaluated for physico-chemical properties like weight variation, hardness, assay friability, in vitro floating behaviour, swelling studies, in vitro dissolution studies and rate order kinetics. Based upon the drug release and floating properties, two formulations (MP04 & MC03) were selected as optimized formulations. The optimized formulations MP04 and MC03 followed zero order rate kinetics, with non-Fickian diffusion and first order rate kinetics with erosion mechanism, respectively. The optimized formulation was characterised with FTIR studies and it was observed that there was no interaction between the drug and polymers.
Formulation and optimization of gastric floating drug delivery system using Central composite design and its biopharmaceutical evaluation

Meka VS, Thing LK, Gorajana A, Kolapalli VR

Pak J Pharm Sci, 2015 Jul;28(4):1373-87.
PMID: 26142528

The present work investigates the formulation and biopharmaceutical estimation of gastric floating drug delivery system (GFDDS) of propranolol HCl using semi-synthetic polymer carboxymethyl ethyl cellulose (CMEC) and a synthetic polymer polyethylene oxide (PEO). A central composite design was applied for optimization of polymer quantity (CMEC or PEO) and sodium bicarbonate concentration as independent variables. The dependent variables evaluated were: % of drug release at 1 hr (D1hr), % drug release at 3 hr (D3hr) and time taken for 95% of drug release (t95). Numerical optimization and graphical optimization were conducted to optimize the response variables. All observed responses of statistically optimized formulations were in high treaty with predicted values. Accelerated stability studies were conducted on the optimized formulations at 40 ± 2°C/75% ± 5% RH and confirm that formulations were stable. Optimized formulations were evaluated for in vivo buoyancy characterization in human volunteers and were found buoyant in gastric fluid. Gastric residence time was enhanced in the fed but not the fasted state. The optimized formulations and marketed formulation were administered to healthy human volunteers and evaluated for pharmacokinetic parameters. Mean residence time (MRT) was prolonged and AUC levels were increased for both optimized floating tablets when compared with marketed product. High relative bioavailability obtained with optimized gastric floating tablets compared to commercial formulation, indicated the improvement of bioavailability.
Fulltext Characterization and in vitro drug release studies of a natural polysaccharide Terminalia catappa gum (Badam gum)

Meka VS, Nali SR, Songa AS, Kolapalli VR

AAPS PharmSciTech, 2012 Dec;13(4):1451-64.
PMID: 23090110 DOI: 10.1208/s12249-012-9873-5

The main objective of the present study is the physicochemical characterization of naturally available Terminalia catappa gum (Badam gum [BG]) as a novel pharmaceutical excipient and its suitability in the development of gastroretentive floating drug delivery systems (GRFDDS) to retard the drug for 12 h when the dosage form is exposed to gastrointestinal fluids in the gastric environment. As BG was being explored for the first time for its pharmaceutical application, physicochemical, microbiological, rheological, and stability studies were carried out on this gum. In the present investigation, the physicochemical properties, such as micromeritic, rheological, melting point, moisture content, pH, swelling index, water absorption, and volatile acidity, were evaluated. The gum was characterized by scanning electron microscopy, differential scanning calorimetry (DSC), powder X-ray diffraction studies (PXRD), and Fourier transform infrared spectroscopy (FTIR). Gastroretentive floating tablets of BG were prepared with the model drug propranolol HCl by direct compression methods. The prepared tablets were evaluated for all their physicochemical properties, in vitro buoyancy, in vitro drug release, and rate order kinetics. PBG 04 was selected as an optimized formulation based on its 12-h drug release and good buoyancy characteristics. The optimized formulation was characterized with FTIR, DSC, and PXRD studies, and no interaction between the drug and BG was found. Thus, the study confirmed that BG might be used in the gastroretentive drug delivery system as a release-retarding polymer.
Thermal sintering: a novel technique in the design of gastroretentive floating tablets of propranolol HCl and its evaluation

Meka VS, Songa AS, Nali SR, Battu JR, Kukati L, Kolapalli VR

Invest Clin, 2012 Sep;53(3):223-36.
PMID: 23248967

The aim of the present investigation was to formulate thermally sintered floating tablets of propranolol HCl, and to study the effect of sintering conditions on drug release, as well as their in vitro buoyancy properties. A hydrophilic polymer, polyethylene oxide, was selected as a sintered polymer to retard the drug release. The formulations were prepared by a direct compression method and were evaluated by in vitro dissolution studies. The results showed that sintering temperature and time of exposure greatly influenced the buoyancy, as well as the dissolution properties. As the sintering temperature and time of exposure increased, floating lag time was found to be decreased, total floating time was increased and drug release was retarded. An optimized sintered formulation (sintering temperature 50 degrees C and time of exposure 4 h) was selected, based on their drug retarding properties. The optimized formulation was characterized with FTIR and DSC studies and no interaction was found between the drug and the polymer used.
Production, Characterization and Evaluation of Kaempferol Nanosuspension for Improving Oral Bioavailability

Qian YS, Ramamurthy S, Candasamy M, Shadab M, Kumar RH, Meka VS

Curr Pharm Biotechnol, 2016;17(6):549-55.
PMID: 26813303

CONTEXT: Kaempferol has a large particle size and poor water solubility, leading to poor oral bioavailability. The present work aimed to develop a kaempferol nanosuspension (KNS) to improve pharmacokinetics and absolute bioavailability.
METHODS: A nanosuspension was prepared using high pressure homogenization (HPH) techniques. The physico-chemical properties of the kaempferol nanosuspension (KNS) were characterized using photon correlation spectroscopy (PCS), transmission electron microscope (TEM), Fourier transform infrared spectroscopy (FTIR) and x-ray diffractometry (XRD). A reversephase high performance liquid chromatography (RP-HPLC) method for the analysis of the drug in rat plasma was developed and validated as per ICH guidelines. In vivo pharmacokinetic parameters of oral pure kaempferol solution, oral kaempferol nanosuspension and intravenous pure kaempferol were assessed in rats.
RESULTS AND DISCUSSION: The kaempferol nanosuspension had a greatly reduced particle size (426.3 ± 5.8 nm), compared to that of pure kaempferol (1737 ± 129 nm). The nanosuspension was stable under refrigerated conditions. No changes in physico-chemical characteristics were observed. In comparison to pure kaempferol, kaempferol nanosuspension exhibited a significantly (P<0.05) increased in Cmax and AUC(0-∞) following oral administration and a significant improvement in absolute bioavailability (38.17%) compared with 13.03% for pure kaempferol.
CONCLUSION: These results demonstrate enhanced oral bioavailability of kaempferol when formulated as a nanosuspension.
Lipid based nanocarriers system for topical delivery of photosensitizers

Md S, Haque S, Madheswaran T, Zeeshan F, Meka VS, Radhakrishnan AK, et al.

Drug Discov Today, 2017 Aug;22(8):1274-1283.
PMID: 28456749 DOI: 10.1016/j.drudis.2017.04.010

Topical photodynamic therapy (PDT) is a non-invasive technique used in the treatment of malignant and non-malignant skin diseases. It offers great promise because of its simplicity, enhanced patient compliance, localisation of the photosensitizer, as well as the use of light and oxygen to achieve photocytotoxicity. Despite progress in photosensitizer-mediated topical PDT, its clinical application is limited by poor penetration of photosensitizers through the skin. Therefore, much effort has been made to develop nanocarriers that can tackle the challenges of conventional photosensitizer-mediated PDT for topical delivery. This review discusses recent data on the use of different types of lipid-based nanocarriers in delivering photosensitizer for topical PDT.
A comprehensive review on polyelectrolyte complexes

Meka VS, Sing MKG, Pichika MR, Nali SR, Kolapalli VRM, Kesharwani P

Drug Discov Today, 2017 11;22(11):1697-1706.
PMID: 28683256 DOI: 10.1016/j.drudis.2017.06.008

Global research on polyelectrolytes at a fundamental and applied level is intensifying because the advantages of sustainability are being accepted in academia and industrial research settings. During recent decades, polyelectrolytes became one of the most attractive subjects of scientific research owing to their great potential in the areas of advanced technologies. Polyelectrolytes are a type of polymer that have multitudinous ionizable functional groups. Ionized polyelectrolytes in solution can form a complex with oppositely charged polyelectrolytes - a polyelectrolyte complex (PEC). The present article provides a comprehensive review on PECs and their classification, theory and characterization, as well as a critical analysis of the current research.
Opportunities for Nano-Formulations in Type 2 Diabetes Mellitus Treatments

Jeevanandam J, Danquah MK, Debnath S, Meka VS, Chan YS

Curr Pharm Biotechnol, 2015;16(10):853-70.
PMID: 26212563 DOI: 10.2174/1389201016666150727120618

Diabetes mellitus has been a threat to humans for many years. Amongst the different diabetes types, type 2 diabetes mellitus is the most common, and this is due to drastic changes in human lifestyle such as lack of exercise, stressful life and so on. There are a large number of conventional treatment methods available for type 2 diabetes mellitus. However, most of these methods are curative and are only applicable when the patient is highly symptomatic. Effective treatment strategies should be geared towards interfering with cellular and bio molecular mechanisms associated with the development and sustenance of the disease. In recent years, research into the medical potential of nanoparticles has been a major endeavor within the pharmaceutical industries. Nanoparticles display unique and tuneable biophysical characteristics which are determined by their shape and size. Nanoparticles have been used to manifest the properties of drugs, and as carriers for drug and vaccine delivery. Notwithstanding, there are further opportunities for nanoparticles to augment the treatment of a wide range of life threatening diseases that are yet to be explored. This review article seeks to highlight the application of potential nano-formulations in the treatment of type 2 diabetes mellitus. In addition, the activity of nanomedicine supplements in reversing insulin resistance is also discussed.
In situ forming phase-inversion implants for sustained ocular delivery of triamcinolone acetonide

Sheshala R, Hong GC, Yee WP, Meka VS, Thakur RRS

Drug Deliv Transl Res, 2019 04;9(2):534-542.
PMID: 29484530 DOI: 10.1007/s13346-018-0491-y

The objectives of this study were to develop biodegradable poly-lactic-co-glycolic acid (PLGA) based injectable phase inversion in situ forming system for sustained delivery of triamcinolone acetonide (TA) and to conduct physicochemical characterisation including in vitro drug release of the prepared formulations. TA (at 0.5%, 1% and 2.5% w/w loading) was dissolved in N-methyl-2-pyrrolidone (NMP) solvent and then incorporated 30% w/w PLGA (50/50 and 75/25) polymer to prepare homogenous injectable solution. The formulations were evaluated for rheological behaviour using rheometer, syringeability by texture analyser, water uptake and rate of implant formation by optical coherence tomography (OCT) microscope. Phase inversion in situ forming formulations were injected into PBS pH 7.3 to form an implant and release samples were collected and analysed for drug content using a HPLC method. All formulations exhibited good syringeability and rheological properties (viscosity: 0.19-3.06 Pa.s) by showing shear thinning behaviour which enable them to remain as free-flowing solution for ease administration. The results from OCT microscope demonstrated that thickness of the implants were increased with the increase in time and the rate of implant formation indicated the fast phase inversion. The drug release from implants was sustained over a period of 42 days. The research findings demonstrated that PLGA/NMP-based phase inversion in situ forming implants can improve compliance in patient's suffering from ocular diseases by sustaining the drug release for a prolonged period of time and thereby reducing the frequency of ocular injections.
Investigation on solution-to-gel characteristic of thermosensitive and mucoadhesive biopolymers for the development of moxifloxacin-loaded sustained release periodontal in situ gels

Sheshala R, Quah SY, Tan GC, Meka VS, Jnanendrappa N, Sahu PS

Drug Deliv Transl Res, 2019 04;9(2):434-443.
PMID: 29392681 DOI: 10.1007/s13346-018-0488-6

The objectives of present research were to develop and characterize thermosensitive and mucoadhesive polymer-based sustained release moxifloxacin in situ gels for the treatment of periodontal diseases. Poloxamer- and chitosan-based in situ gels are in liquid form at room temperature and transform into gel once administered into periodontal pocket due to raise in temperature to 37 °C. Besides solution-to-gel characteristic of polymers, their mucoadhesive nature aids the gel to adhere to mucosa in periodontal pocket for prolonged time and releases the drug in sustained manner. These formulations were prepared using cold method and evaluated for pH, solution-gel temperature, syringeability and viscosity. In vitro drug release studies were conducted using dialysis membrane at 37 °C and 50 rpm. Antimicrobial studies carried out against Aggregatibacter actinomycetemcomitans (A.A.) and Streptococcus mutans (S. Mutans) using agar cup-plate method. The prepared formulations were clear and pH was at 7.01-7.40. The viscosity of formulations was found to be satisfactory. Among the all, formulations comprising of 21% poloxamer 407 and 2% poloxamer 188 (P5) and in combination with 0.5% HPMC (P6) as well as 2% chitosan and 70% β-glycerophosphate (C6) demonstrated an ideal gelation temperature (33-37 °C) and sustained the drug release for 8 h. Formulations P6 and C6 showed promising antimicrobial efficacy with zone of inhibition of 27 mm for A.A. and 55 mm for S. Mutans. The developed sustained release in situ gel formulations could enhance patient's compliance by reducing the dosing frequency and also act as an alternative treatment to curb periodontitis.
Application of diverse natural polymers in the design of oral gels for the treatment of periodontal diseases

Ganguly A, Ian CK, Sheshala R, Sahu PS, Al-Waeli H, Meka VS

J Mater Sci Mater Med, 2017 Mar;28(3):39.
PMID: 28144851 DOI: 10.1007/s10856-017-5852-4

The objective of this study was to prepare periodontal gels using natural polymers such as badam gum, karaya gum and chitosan. These gels were tested for their physical and biochemical properties and assessed for their antibacterial activity against Aggregatibacter actinomycetemcomitans and Streptococcus mutans, two pathogens associated with periodontal disease. Badam gum, karaya gum and chitosan were used to prepare gels of varying concentrations. Moxifloxacin hydrochloride, a known antimicrobial drug was choosen in the present study and it was added to the above gels. The gels were then run through a battery of tests in order to determine their physical properties such as pH and viscosity. Diffusion studies were carried out on the gels containing the drug. Antimicrobial testing of the gels against various bacteria was then carried out to determine the effectiveness of the gels against these pathogens. The results showed that natural polymers can be used to produce gels. These gels do not have inherent antimicrobial properties against A. actinomycetemcomitans and S. mutans. However, they can be used as a transport vehicle to carry and release antimicrobial drugs.
Recent Advances in Non-Invasive Delivery of Macromolecules using Nanoparticulate Carriers System

Shadab M, Haque S, Sheshala R, Meng LW, Meka VS, Ali J

Curr Pharm Des, 2017;23(3):440-453.
PMID: 27784250 DOI: 10.2174/1381612822666161026163201

BACKGROUND: The drug delivery of macromolecules such as proteins and peptides has become an important area of research and represents the fastest expanding share of the market for human medicines. The most common method for delivering macromolecules is parenterally. However parenteral administration of some therapeutic macromolecules has not been effective because of their rapid clearance from the body. As a result, most macromolecules are only therapeutically useful after multiple injections, which causes poor compliance and systemic side effects.
METHOD: Therefore, there is a need to improve delivery of therapeutic macromolecules to enable non-invasive delivery routes, less frequent dosing through controlled-release drug delivery, and improved drug targeting to increase efficacy and reduce side effects.
RESULT: Non-invasive administration routes such as intranasal, pulmonary, transdermal, ocular and oral delivery have been attempted intensively by formulating macromolecules into nanoparticulate carriers system such as polymeric and lipidic nanoparticles.
CONCLUSION: This review discusses barriers to drug delivery and current formulation technologies to overcome the unfavorable properties of macromolecules via non-invasive delivery (mainly intranasal, pulmonary, transdermal oral and ocular) with a focus on nanoparticulate carrier systems. This review also provided a summary and discussion of recent data on non-invasive delivery of macromolecules using nanoparticulate formulations.
Fulltext Statistical optimization of a novel excipient (CMEC) based gastro retentive floating tablets of propranolol HCl and it's in vivo buoyancy characterization in healthy human volunteers

Meka VS, Nali SR, Songa AS, Battu JR, Kolapalli VR

Daru, 2012 Aug 30;20(1):21.
PMID: 23351981 DOI: 10.1186/2008-2231-20-21

The objective of the present investigation is to formulate gastro retentive floating drug delivery systems (GRFDDS) of propranolol HCl by central composite design and to study the effect of formulation variables on floating lag time, D1hr (% drug release at 1 hr) and t90 (time required to release 90% of the drug). 3 factor central composite design was employed for the development of GRFDDS containing novel semi synthetic polymer carboxymethyl ethyl cellulose (CMEC) as a release retarding polymer. CMEC, sodium bicarbonate and Povidone concentrations were included as independent variables. The tablets were prepared by direct compression method and were evaluated for in vitro buoyancy and dissolution studies. From the polynomial model fitting statistical analysis, it was confirmed that the response floating lag time and D1hr is suggested to quadratic model and t90 is suggested to linear model. All the statistical formulations followed first order rate kinetics with non-Fickian diffusion mechanism. The desirability function was used to optimize the response variables, each having a different target, and the observed responses were highly agreed with experimental values. Statistically optimized formulation was characterized by FTIR and DSC studies and found no interactions between drug and polymer. The results demonstrate the feasibility of the model in the development of GRFDDS containing a propranolol HCl. Statistically optimized formulation was evaluated for in vivo buoyancy studies in healthy humans for both fed and fasted states. From the results, it was concluded that gastric residence time of the floating tablets were enhanced at fed stage but not in fasted state.

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